BRPI0900802A2 - essential oils and compounds isolated from baccharis spp. extracts, pharmaceutical and / or cosmetic formulations and their uses - Google Patents
essential oils and compounds isolated from baccharis spp. extracts, pharmaceutical and / or cosmetic formulations and their uses Download PDFInfo
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- BRPI0900802A2 BRPI0900802A2 BRPI0900802A BRPI0900802A2 BR PI0900802 A2 BRPI0900802 A2 BR PI0900802A2 BR PI0900802 A BRPI0900802 A BR PI0900802A BR PI0900802 A2 BRPI0900802 A2 BR PI0900802A2
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- pharmaceutical
- essential oils
- compounds
- formulations
- isolated
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Abstract
ËLEOS ESSENCIAIS E COMPOSTOS ISOLADOS DE EXTRATOS DE BACCHARIS SPP., FORMULAçõES FARMACêUTICAS E/OU COSMéTICAS E SEUS USOS A presente invenção refere-se a óleos essenciais e/ou compostos isolados de extratos de Baccharis spp., preferencialmente, Baccharis dracunculifolia D.C. Adicionalmente o presente pedido provê formulações farmacêuticas e/ou cosméticas, preferencialmente, microemulsões contendo o dito óleo essencial e/ou compostos isolados aplicados como agentes analgésicos, antiinflamatórios, cicatrizantes, antibacteriano, anticariogênico ei ou antineoplásicos,preferencialmente, como agentes para saúde bucal.ESSENTIAL OILS AND COMPOUNDS ISOLATED FROM BACCHARIS SPP. EXTRACTS, PHARMACEUTICAL AND / OR COSMETIC FORMULATIONS AND THEIR USES The present invention relates to essential oils and / or compounds isolated from extracts of Baccharis spp., Preferably Baccharis dracunculifolia DC. The present invention provides pharmaceutical and / or cosmetic formulations, preferably microemulsions containing said essential oil and / or isolated compounds applied as analgesic, anti-inflammatory, scarring, antibacterial, anti-cariogenic or anti-neoplastic agents, preferably as oral health agents.
Description
"ÓLEOS ESSENCIAIS E COMPOSTOS ISOLADOS DE EXTRATOS DEBACCHARIS SPP., FORMULAÇÕES FARMACÊUTICAS E/OUCOSMÉTICAS E SEUS USOS""ESSENTIAL OILS AND COMPOUNDS ISOLATED FROM DEBACCHARIS SPP. EXTRACTS, PHARMACEUTICAL AND / OUCOSMETIC FORMULATIONS AND THEIR USES"
Campo da InvençãoField of the Invention
A presente invenção refere-se a óleos essenciais e/oucompostos isolados de extratos de Baccharis spp., preferencialmente,Baeeharis dracuneulifolia D.C. Adicionalmente o presente pedido provêformulações farmacêuticas e/ou cosméticas, preferencialmente,microemulsões contendo o dito óleo essencial e/ou compostos isoladosaplicados como agentes analgésicos, antiinflamatórios, cicatrizantes,antibacteriano, anticariogênico e/ou antineoplásicos,preferencialmente, como agentes para saúde bucal.The present invention relates to essential oils and / or compounds isolated from Baccharis spp. Extracts, preferably Baeeharis dracuneulifolia DC. Additionally the present application provides pharmaceutical and / or cosmetic formulations, preferably microemulsions containing said essential oil and / or isolated compounds as applied. analgesic, anti-inflammatory, healing, antibacterial, anti-cariogenic and / or antineoplastic agents, preferably as agents for oral health.
Antecedentes da InvençãoBackground of the Invention
O gênero Baeeharis (família Asteraceae, tribo Astereae) estárepresentado por mais de 500 espécies distribuídas principalmente empaíses sul-americanos. No Brasil estão descritas 120 espécies deBaeeharis, com a maior parte delas localizadas na região sudeste dopaís. A grande concentração de espécies no Brasil, principalmente nocerrado e bordas da Mata Atlântica, indicam que estas regiões sãopossíveis centros de origem do gênero e devido à sua importânciamedicinal, comercial e ecológica, várias espécies de Baeeharis têmatraído a atenção de pesquisadores das áreas de fitoquímica,farmacologia e biologia.The genus Baeeharis (family Asteraceae, tribe Astereae) is represented by over 500 species distributed mainly in South American countries. In Brazil, 120 species of Baeeharis are described, most of them located in the southeastern region of Brazil. The high concentration of species in Brazil, mainly in the Atlantic Forest and edges of the Atlantic Forest, indicate that these regions are possible centers of origin of the genus and due to their medical, commercial and ecological importance, several species of Baeeharis have attracted the attention of researchers from the phytochemical areas. pharmacology and biology.
Espécies do gênero Baeeharis têm reputado uso namedicina caseira de países latino-americanos, sendo consumidasprincipalmente na forma de chás com indicações para disfunçõesgástricas e hepáticas, anemias, inflamações, diabetes ou doenças napróstata.Quimicamente a família Bacchans se destaca pela enormediversidade de metabólitos secundários, sendo caracterizado pelapresença de terpenóides, especialmente, triterpenos, diterpenosclerodanos e labdanos, flavonóides, especialmente, flavonas e flavonóis,fenilprenilados derivados do ácido p-cumárico e poliacetilenos. Seusprincipais metabólitos possuem ampla diversidade estrutural evariedade de atividades biológicas comprovadas, tais como atividadeantitumoral, antioxidante, repelente de insetos, tripanocida eantiinflamatória.Species of the genus Baeeharis have been reputed to use homemade medicine from Latin American countries, being consumed mainly in the form of teas with indications for gastric and liver dysfunction, anemia, inflammation, diabetes or nausea. Chemically, the Bacchans family stands out for the huge diversity of secondary metabolites. characterized by the presence of terpenoids, especially triterpenes, diterpenosclerodans and labdans, especially flavonoids, flavones and flavonols, phenylprenylated p-coumaric acid derivatives and polyacetylenes. Its main metabolites have a wide structural diversity and variety of proven biological activities, such as tumor activity, antioxidant, insect repellent, and anti-inflammatory trypanocide.
Particularmente, Baceharis dracunculifolia DC,popularmente conhecida como alecrim-do-campo ou vassoura, é umarbusto nativo das regiões sudeste e sul do Brasil, ocorrendo em áreasde solo pobre e pastagens abandonadas. É particularmente utilizada, namedicina popular, como antiinflamatório, cicatrizante e no tratamentode transtornos gastrointestinais. O decoto das folhas também é usadocomo antipirético. Algumas propriedades medicinais do extrato purodesta espécie já foram comprovadas, incluindo atividades tripanocida,antiulcerogênica, antimutagênica, e imunomoduladora.In particular, Baceharis dracunculifolia DC, popularly known as field rosemary or broom, is a shrub native to southeastern and southern Brazil, occurring in areas of poor soil and abandoned pastures. It is particularly used, named popularicin, as anti-inflammatory, healing and in the treatment of gastrointestinal disorders. The leaf cleavage is also used as antipyretic. Some medicinal properties of the extract of this species have been proven, including trypanocidal, antiulcerogenic, antimutagenic, and immunomodulatory activities.
O óleo essencial de B. dracunculifolia também tem sidoestudado, devido ao seu aroma exótico, forte e duradouro, o qual éaltamente valorizado pela indústria de perfumes.The essential oil of B. dracunculifolia has also been studied due to its strong, long lasting exotic aroma which is highly valued by the perfume industry.
Suas folhas e principalmente os ápices foliares sãodensamente pontuados por tricomas glandulares, estruturas de grandeimportância na interação desta espécie com insetos, especialmenteabelhas. De acordo com diversos autores, B. dracunculifolia é aprincipal fonte botânica da própolis verde, uma variedade de própolisbrasileira, preparada por abelhas (Apis mellifera africanizadas) a partirdo processamento dos ápices vegetativos desta planta.A própolis verde, por sua vez, vem se tornando cada vezmais popular, no Japão, Estados Unidos da América, China e paísesintegrantes da comunidade européia em virtude de suas reconhecidaspropriedades medicinais, incluindo atividades analgésica,antiinflamatória, antiulcerogênica, antibacteriana, atuando tambémcomo neuroprotetor e prevenindo o desenvolvimento de determinadostipos de câncer.Its leaves and especially the leaf apex are heavily punctuated by glandular trichomes, structures of great importance in the interaction of this species with insects, especially bees. According to several authors, B. dracunculifolia is the main botanical source of green propolis, a variety of Brazilian propolis, prepared by bees (Apis mellifera africanizada) from the processing of the vegetative apexes of this plant. Green propolis, in turn, has become increasingly popular in Japan, the United States of America, China, and member countries of the European community because of their recognized medicinal properties, including analgesic, anti-inflammatory, antiulcerogenic, antibacterial activities, also acting as a neuroprotective agent and preventing the development of certain types of cancer.
Existem relatos de que os extratos puros de B.dracunculifolia apresentam efeito imunomodulatória, ativandomacrófagos com conseqüente liberação de peróxido de hidrogênio einduzindo a produção de formas reativas de oxigênio em neutrófilosestimulados, dentro de um perfil dose-dependente. O extratohidroetanólico de B. dracunculifolia também apresentou propriedadeantiulcerogênica com eficácia semelhante ao da cimetidina ouomeprazol, em cobaias, diminuindo significativamente os índices delesões da mucosa gástrica, a área total de lesão e a porcentagem delesões, em comparação aos grupos-controle. O extrato vegetal tambémreduziu o volume de suco gástrico e a acidez total, ocasionandoaumento do pH gástrico (KLOPELL F.C., LEMOS M., SOUSA J.P.,COMUNELLO E., MAISTRO E.L., BASTOS J.K., DE ANDRADE S.F.Nerolidol, an antiulcer constituent from the essential oil of Baccharisdracunculifolia DC (Asteraceae). Z Naturforsch [C], 2007 Jul-Aug;62(7-8):537-42.).Pure extracts of B.dracunculifolia have been reported to have immunomodulatory effect, activating macrophages with consequent release of hydrogen peroxide and inducing the production of reactive oxygen forms in stimulated neutrophils within a dose-dependent profile. B. dracunculifolia hydrohydethanolic extract also had an anti-cancer property with similar efficacy to cimetidine or meprazole in guinea pigs, significantly decreasing gastric mucosa deletion rates, total lesion area and percentage of lesions compared to control groups. The plant extract also reduced gastric juice volume and total acidity, causing an increase in gastric pH (KLOPELL FC, LEMOS M., SOUSA JP, COMMUNEL E., MAISTRO EL, BASTOS JK, ANDRADE SFNerolidol, an antiulcer constituent from the essential oil of Baccharisdracunculifolia DC (Asteraceae) Z Naturforsch [C], 2007 Jul-Aug; 62 (7-8): 537-42.).
A formação de microestruturas em soluções aquosas detensoativos é um fenômeno comum de auto-organização molecularcomo forma de atingir a estabilidade termodinâmica. Esse fenômenotorna-se a base para a aplicação tecnológica dos tensoativos comosistemas organizados nas ciências biológicas.Nos últimos anos a procura por novos sistemas de liberaçãode fármacos tem sido muito relevante no sentido de se estabeleceralternativas terapêuticas mais eficientes, que possibilitem administraros fármacos com mais segurança e com efeitos colaterais minimizados.The formation of microstructures in detensive aqueous solutions is a common phenomenon of molecular self-organization as a way to achieve thermodynamic stability. This phenomenon has become the basis for the technological application of surfactants as organized systems in the biological sciences. In recent years the search for new drug delivery systems has been very relevant in order to establish more efficient therapeutic alternatives, which enable the administration of drugs more safely and effectively. with minimized side effects.
Pesquisas avançadas têm sido realizadas concernentes aossistemas micro e nanoestruturados de tensoativos, por sua capacidadeem aumentar a eficácia terapêutica de fármacos, permitindo a reduçãoda dose administrada e minimizando os efeitos colaterais potenciais dosfármacos. Os sistemas micro e nanoemulsionados são capazes decompartimentalizar fármacos nas gotículas da fase interna, as quaispossuem propriedades físico-químicas bastante diferentes das do meiodispersante, induzindo modificações nas propriedades biológicas dosfármacos incorporados. Além disso, esses sistemas melhoram asolubilização de fármacos lipofílicos em água e os protegem contrahidrólise enzimática, além de aumentar o potencial de absorção devidoà presença de tensoativo.Advanced research has been performed concerning the microstructured and nanostructured surfactant systems, for their ability to increase the therapeutic efficacy of drugs, allowing the reduction of the administered dose and minimizing the potential side effects of the drugs. Micro and nanoemulsion systems are able to de-compartmentalize drugs in the internal phase droplets, which have physicochemical properties quite different from those of the meiodispersant, inducing modifications in the biological properties of the incorporated drugs. In addition, these systems improve the solubilization of lipophilic drugs in water and protect them against enzymatic hydrolysis, and increase their absorption potential due to the presence of surfactant.
Em particular, as doenças dentais estão entre as maisprevalentes e onerosas nas sociedades industrializadas. A cárie dental éum dos processos infecciosos crônicos da cavidade bucal maissignificativo em seres humanos, cuja causa multifatorial envolve ascaracterísticas físicas da cavidade bucal, a capacidade tamponantesalivar, as espécies de microrganismos que integram a microbiotabucal, bem como, os desequilíbrios ecológicos sofridos por estamicrobiota em resposta ao aumento do consumo de carboidratosfermentáveis na dieta alimentar.In particular, dental diseases are among the most prevalent and costly in industrialized societies. Tooth decay is one of the most significant chronic infectious processes of the oral cavity in humans, whose multifactorial cause involves the physical characteristics of the oral cavity, the tamponantesalivar capacity, the species of microorganisms that integrate the microbiotabucal, as well as the ecological imbalances suffered by stamicrobiotic in response. increased intake of fermentable carbohydrates in the diet.
Dentre os fatores primários, a placa dental bacteriana éconsiderada o principal fator etiológico para o desenvolvimento de cáriese doenças periodontais. Trata-se de uma película incolor, aderente enão mineralizada, composta por diversas espécies bacterianas,sustentadas por uma matriz de proteínas salivares, polissacarídeos,células descarnadas, leucócitos e restos alimentares, que se forma sobrea superfície dos dentes e tecidos gengivais em diferentes sítios dacavidade bucal.Among the primary factors, dental plaque is considered the main etiological factor for the development of periodontal disease. It is a colorless, adherent, non-mineralized film composed of several bacterial species, supported by a matrix of salivary proteins, polysaccharides, fleshless cells, leukocytes, and food debris, which forms on the surface of teeth and gingival tissues at different sites of cavity. oral.
Mas, ao contrário do que se possa supor, a colonizaçãomicrobiana dos dentes pode ser benéfica, na medida em que contribuipara a defesa da cavidade bucal contra a instalação de microrganismospatogênicos, através de mecanismos de competição. Portanto, aformação de uma placa dental patogênica irá ocorrer sempre que oequilíbrio ecológico for quebrado, e a composição e as atividadesmetabólicas desta complexa comunidade que compõe a placa dentalforem modificadas.However, contrary to what may be supposed, the microbial colonization of the teeth may be beneficial, as it contributes to the defense of the oral cavity against the installation of pathogenic microorganisms through mechanisms of competition. Therefore, the formation of a pathogenic dental plaque will occur whenever the ecological balance is broken, and the composition and metabolic activities of this complex community that makes up the dental plaque have been modified.
O controle da placa dental é a chave para a prevenção damaioria das doenças da cavidade bucal, especialmente cáries e doençasperiodontais, constituindo, ainda, um alvo para reduzir formação demanchas e cálculos dentais. Mesmo com o uso de escovas de dente emcombinação com dentifrícios convencionais contendo 0,2% de fluoretode sódio não é o bastante para remover toda a placa, especialmenteaquela que se forma nas margens gengivais, espaços inter-proximais efissuras dos dentes. Conseqüentemente, medidas adicionais para ocontrole da placa são necessárias. Agentes quimioterapêuticos,adicionados a dentifrícios, enxaguatórios bucais e outras formulaçõesodontológicas incluem agentes quelantes que podem afetar ascaracterísticas físico-químicas da película salivar, sistemas detergentesque podem dispersar ou desprender a placa, e agentes antimicrobianosque reduzem a patogenicidade da placa dental remanescente, aderida aos dentes.The control of dental plaque is the key to preventing most oral cavity diseases, especially dental caries and periodontal diseases, and is also a target to reduce the formation of dental stains and calculi. Even using toothbrushes in combination with conventional toothpastes containing 0.2% sodium fluoride is not enough to remove all the plaque, especially the one that forms on the gingival margins, inter-proximal and fissure spaces of the teeth. Consequently, additional measures for board control are required. Chemotherapeutic agents, added to dentifrices, mouthwashes and other dental formulations include chelating agents that may affect the physicochemical characteristics of salivary film, detergent systems that may disperse or detach plaque, and antimicrobial agents that reduce the pathogenicity of the remaining dental plaque adhered to teeth.
Atualmente várias tentativas para se eliminar espéciespatogênicas da microbiota bucal, com antibióticos, por exemplo,ampicilina, eritromicina, penicilina, tetraciclina e vancomicina semostram muito efetivas na prevenção da cárie dental. Todavia, o usoexcessivo destes fármacos pode ocasionar desarranjos na microbiotaoral e intestinal e causar efeitos colaterais indesejáveis tais comosusceptibilidade a microrganismos, vômitos, diarréias e manchamentodos dentes.Currently several attempts to eliminate pathogenic species of the oral microbiota with antibiotics, for example ampicillin, erythromycin, penicillin, tetracycline and vancomycin have been shown to be very effective in preventing dental caries. However, excessive use of these drugs may cause breakdowns in the oral and intestinal microbiota and cause undesirable side effects such as susceptibility to microorganisms, vomiting, diarrhea and staining of teeth.
Sanguinarina, um alcalóide isolado dos rizomas deSanguinana canadensis, que exibe um efeito antibacteriano de amploespectro sobre bactérias bucais, tem sido usado como agenteanticariogênico em uma grande variedade de produtos para higienebucal, tais como, dentifrícios e enxaguatórios bucais, devido à sua altaeficácia. A sua aplicação industrial, porém, foi acentuadamentereduzida, devido a relatos de que sanguinarina estaria associada acasos de leucoplaquia oral, uma condição da cavidade bucal queenvolve a formação de manchas brancas e fibrosas que se desenvolve nalíngua ou na parte interna da bochecha como resposta a uma irritaçãocrônica.Sanguinarina, an alkaloid isolated from the rhizomes of Sanguinana canadensis, which exhibits a broad-spectrum antibacterial effect on oral bacteria, has been used as an antiogenic agent in a wide variety of hygiene products such as toothpastes and mouthwash due to its high efficacy. Its industrial application, however, has been markedly reduced due to reports that sanguinarine is associated with oral leukoplakia, a condition of the oral cavity that develops the formation of white and fibrous patches that develop on the tongue or inside the cheek in response to a chronic irritation.
O agente antimicrobiano mais eficaz usado, atualmente, nocontrole da cárie dental é a clorohexedina, uma bisbiguanida catiônicasintética que apresenta uma molécula simétrica, consistindo de doisanéis 4-clorofenil e dois grupos biguanida conectados por uma cadeiade hexametileno central (1, Γ-hexametilenobis [5-(p-clorofenil)biguanida]). Tal composto pode se apresentar na forma de diversos sais,tais como, gluconato, digluconato, acetato e hidrocloridrato, mas o salde digluconato é a forma mais indicada, por apresentar maiorsolubilidade em meio aquoso e no pH fisiológico, dissociando-se paraliberar o componente catiônico. Ainda, comprovou-se que o compostoreduz a incidência da cárie em animais e humanos. O compostotambém é capaz de inibir a formação de ácidos no biofilme jáestabelecido, por algumas horas, após uma aplicação na concentraçãode 0,2%. A clorohexedina possui, ainda, alta afinidade pelahidroxipatita do esmalte dental e seu elevado poder de retenção nacavidade bucal explica os seus efeitos clínicos prolongados. Emconcentrações relativamente altas, a clorohexedina pode eliminarparcialmente o biofilme bacteriano e afetar, até certo ponto, ometabolismo das bactérias remanescentes. Porém, apesar de eficienteno combate à cárie dental, a clorohexedina apresenta efeitos adversos,causando o aparecimento de manchas marrons na superfície dental,além de deixar gosto metálico na boca, provocar náuseas e vômitos,dores abdominais, hipersalivação e desensibilização das papilasgustativas com conseqüente perda do paladar.The most effective antimicrobial agent currently used in dental caries control is chlorhexedine, a cationic synthetic bisbiguanide that has a symmetrical molecule consisting of two 4-chlorophenyl rings and two biguanide groups connected by a central hexamethylene chain (1, Γ-hexamethylenebis [5 - (p-chlorophenyl) biguanide]). Such compound may be in the form of several salts, such as gluconate, digluconate, acetate and hydrochloride, but the digluconate salt is the most suitable form, because it has higher solubility in aqueous medium and physiological pH, dissociating paralyzing the cationic component. . Still, it has been proven that the compound reduces the incidence of caries in animals and humans. Compost is also able to inhibit acid formation in the already established biofilm for a few hours after application at a concentration of 0.2%. Chlorhexedine also has a high affinity for dental enamel hydroxypatite and its high retention power in oral cavity explains its prolonged clinical effects. At relatively high concentrations, chlorhexedine can partially eliminate bacterial biofilm and affect to some extent the remaining bacteria ometabolism. However, despite the effective fight against dental caries, chlorhexedine has adverse effects, causing the appearance of brown spots on the dental surface, besides leaving metallic taste in the mouth, causing nausea and vomiting, abdominal pain, hypersalivation and desensitization of the papillae with consequent loss. of taste.
Outros processos infecciosos crônicos que afetam acavidade bucal são as chamadas doenças periodontais, que abrangemas gengivites e as periodontites. Cerca de 3 em cada 4 pessoas sofremdestas doenças, e ao redor de 10% da população parece sofrer dasformas mais severas, sendo provocadas principalmente por bactérias daplaca bacteriana subgengival. As gengivites envolvem a inflamação dagengiva enquanto as periodontites provocam infecção de todos ostecidos periodontais.Other chronic infectious processes that affect oral cavity are called periodontal diseases, which include gingivitis and periodontitis. About 3 out of 4 people suffer from these diseases, and around 10% of the population appears to suffer from the most severe deformities, mainly caused by subgingival bacterial plaque bacteria. Gingivitis involves dagengive inflammation while periodontitis causes infection of all periodontal ostensates.
Estudos mais recentes indicam, ainda, que as doençasperiodontais constituem um fator de risco para as doençascardiovasculares, na medida em que os microrganismos alojados nabolsa periodontal têm acesso à corrente sangüínea. Também podem sertransmitidas entre familiares através do compartilhamento de talheres eoutros fômites.More recent studies also indicate that periodontal diseases constitute a risk factor for cardiovascular diseases, as microorganisms housed in periodontal pockets have access to the bloodstream. They can also be transmitted to family members by sharing cutlery and other formats.
Marcadores genéticos de DNA indicam que famílias que têmpessoas com doença periodontal avançada, apresentam 30% de chancede apresentar a doença também, com futura perda dos dentes, se nãohouver tratamento. O tratamento periodontal consiste de procedimentosde raspagem da base dos dentes (bolsa periodontal), visando ahigienização dos tecidos e remoção da placa bacteriana. Em quadrosmais avançados, o tratamento cirúrgico e a antibióticoterapia sãoindicados. Mas já foi demonstrado que após 2 ou 3 anos o paciente nãosupervisionado volta a manifestar a doença. Portanto, a prevençãodestas doenças é o mais recomendável, evitando-se a formação de placadentária através de uma higienização eficaz.Genetic DNA markers indicate that families who have people with advanced periodontal disease have a 30% chance of having the disease as well, with future loss of teeth if there is no treatment. Periodontal treatment consists of scraping procedures of the base of the teeth (periodontal pocket), aiming at tissue hygiene and plaque removal. In more advanced cases, surgical treatment and antibiotic therapy are indicated. But it has been shown that after 2 or 3 years the non-supervised patient again manifests the disease. Therefore, the prevention of these diseases is the most recommended, avoiding the formation of placental through effective hygiene.
Assim, diante de tais limitações, torna-se necessária abusca por novos agentes terapêuticos naturais que sejam eficazes e semostrem seguros para seres humanos.Thus, in the face of such limitations, it is necessary to search for new natural therapeutic agents that are effective and safe for humans.
Microemulsões (ME) podem ser definidas como sistemastermodinamicamente estáveis, isotrópicos, transparentes, de doislíquidos imiscíveis, usualmente água e óleo, estabilizados por um filmede compostos tensoativos, localizados na interface óleo/água.Microemulsions (ME) can be defined as thermodynamically stable, isotropic, transparent, immiscible two-liquid, usually water and oil systems, stabilized by a surfactant film located at the oil / water interface.
Entretanto, a possibilidade de formar microemulsão depende dobalanço entre as propriedades hidrofílicas e lipofílicas do tensoativo,determinada não somente pela sua estrutura química, mas também poroutros fatores como temperatura, força iônica e a presença de co-tensoativo. A mistura de tensoativos com equilíbrio hidrófllo-lipófiloadequado proporciona a condição máxima de "solubilização" do óleo eda água. Assim, a formação da microemulsão geralmente envolve acombinação de três a cinco componentes, tais como tensoativo, água,óleo e, quando necessário, o co-tensoativo, sendo que a orientação parasistemas O/A ou A/O é dependente das propriedades físico-químicas dotensoativo e do óleo, da relação entre as proporções tensoativo/co-tensoativo e entre as proporções água/óleo.However, the possibility of forming microemulsion depends on the balance between the surfactant's hydrophilic and lipophilic properties, determined not only by its chemical structure, but also by other factors such as temperature, ionic strength and the presence of co-surfactant. Mixing surfactants with suitable hydrophilic-lipophilic balance provides the maximum condition for "solubilization" of oil and water. Thus, the formation of microemulsion generally involves the combination of three to five components, such as surfactant, water, oil and, where necessary, co-surfactant, with O / A or A / O orientation being dependent on the physicochemical properties. chemical and oil, the relationship between the surfactant / co-surfactant ratio and the water / oil ratio.
A principal característica desses sistemas é formar umaemulsão muito fina por homogeneização suave com fase aquosa, cujasdimensões das gotículas da fase interna é da ordem de nanômetros. Asmicroemulsões são superiores às soluções micelares em termos depotencial de solubilização de substâncias, por isso, são usadas paraaumentar a solubilização e a absorção de fármacos lipofílicos. Suaestabilidade termodinâmica oferece vantagens sobre as dispersõesinstáveis, tais como as suspensões e emulsões, possuindo tempo devida útil muito mais amplo.The main feature of these systems is to form a very fine emulsion by smooth homogenization with aqueous phase, whose internal phase droplet dimensions are of the order of nanometers. Microemulsions are superior to micellar solutions in terms of substance solubilization potential, so they are used to increase the solubilization and absorption of lipophilic drugs. Its thermodynamic stability offers advantages over unstable dispersions, such as suspensions and emulsions, having much longer working time.
Nos últimos anos, tem aumentado o interesse na aplicaçãode microemulsões como sistema de liberação de fármacos, já que essesagregados apresentam-se descritos na literatura como sistemasreservatórios e permitem liberação lenta do fármaco, a qual proporcionaefeito prolongado, evitando atingir concentração plasmática acima donecessário.In recent years, there has been increasing interest in the application of microemulsions as a drug delivery system, since these aggregates have been described in the literature as reservoir systems and allow slow release of the drug, which provides prolonged effect, avoiding reaching plasma concentration above the required.
Dispersões coloidais óleo em água representam interessanteperspectiva para o desenvolvimento de formulações, pois estas sãoutilizadas como veículos para liberação de fármacos pouco solúveis emágua.Oil-in-water colloidal dispersions represent an interesting prospect for the development of formulations, as these are used as vehicles for the release of drugs that are poorly soluble in water.
Considerando a baixa solubilidade dos extratos, frações edeterminados componentes ativos de B. dracunculifolia em veículosaquosos, tornou-se necessário o desenvolvimento de novos sistemasmicro/nanoemulsionados para a apropriada solubilização, veiculação eliberação dos produtos naturais (ativos) em sítios biológicos específicos,lançando mão de combinações planejadas de tensoativos.Considering the low solubility of extracts, fractions and certain active components of B. dracunculifolia in vehicular whey, it became necessary to develop new micro / nanoemulsion systems for the appropriate solubilization, delivery and release of natural (active) products at specific biological sites, using planned combinations of surfactants.
Diante de todo o exposto, a Depositante inovou, de formainesperada, a caracterização dos óleos essenciais e isolados do extratode Baccharis e sua aplicação em formas farmacêuticas e cosméticas emnanotecnologias.Given all of the above, the Depositor has unexpectedly innovated the characterization of the essential oils and isolates of the Baccharis extract and their application in pharmaceutical and cosmetic forms in nanotechnologies.
Descrição das FigurasDescription of the Figures
A figura 1 mostra o fluxograma geral do procedimento deformulação dos produtos.Figure 1 shows the general flow chart of the product deformulation procedure.
A figura 2 apresenta o diagrama de fases para obtenção dosprodutos semi-acabados, porém, não sendo limitativo.Figure 2 presents the phase diagram for obtaining the semi-finished products, but it is not limiting.
Descrição da InvençãoDescription of the Invention
A presente invenção refere-se a óleos essenciais e/oucompostos isolados de extratos de Baccharis spp., preferencialmente,Baeeharis dracuneulifolia D.C. Adicionalmente o presente pedido provêformulações farmacêuticas e/ou cosméticas, preferencialmente,microemulsões contendo o dito óleo essencial e/ou compostos isoladosaplicados como agentes analgésicos, antiinflamatórios, cicatrizantes,antibacteriano, anticariogênico e/ou antineoplásicos,preferencialmente, como agentes para saúde bucal.The present invention relates to essential oils and / or compounds isolated from Baccharis spp. Extracts, preferably Baeeharis dracuneulifolia DC. Additionally the present application provides pharmaceutical and / or cosmetic formulations, preferably microemulsions containing said essential oil and / or isolated compounds as applied. analgesic, anti-inflammatory, healing, antibacterial, anti-cariogenic and / or antineoplastic agents, preferably as agents for oral health.
Em uma primeira realização a presente invenção refere-se aóleos essenciais e/ou seus compostos isolados de extratos de Baceharisspp, como por exemplo, terpenos, flavonóides e/ou fenilpropanóides.Ainda, o presente pedido de patente classifica os seus compostosisolados em dois grupos: compostos majoritários, particularmente,ácido caféico, ácido ferúlico, isosakuranetina, aromadendrina-4'-metiléter, bacarina, e artepilin C e como compostos minoritários, comopor exemplo, viscidona, friedelanol, lactona de ácido hautriwaico e ácidoursólico.In a first embodiment the present invention relates to essential oils and / or their compounds isolated from Baceharisspp extracts, such as terpenes, flavonoids and / or phenylpropanoids. Further, the present patent application classifies its isolated compounds into two groups: major compounds, in particular caffeic acid, ferulic acid, isosakuranetine, aromadendrin-4'-methylether, baccarin, and artepilin C and as minority compounds, such as viscidone, friedelanol, hautriwaic acid lactone and acidic.
As espécies de Baccharis da presente invenção podem serescolhidas entre B. trimera, B.articulata. B. stenoeephala, B. tridentata,B. mierodonta, B. ligustrina, B. pseudotenuifolia, B. platipuda, B. crispa,B. mieroeephala, B. myrioeephala, B. usterii, B. dentata, B. diseolor, B.eliptiea, B. erioelada, B. fastigiata, B. graeilis, B. juneiformis, B. lundii, B.martiana, B. mínutiflora, B. multisuleata, B. opuntioides, B. pentziaefolia,B. platypoda, B. serrulata, B. subdentada, B. tarchonanthoides, B.vernonioides, entre outros, preferencialmente, Baceharis dracuneulifoliaD.C.Baccharis species of the present invention may be chosen from B. trimera, B.articulata. B. stenoeephala, B. tridentata, B. mierodonta, B. ligustrina, B. pseudotenuifolia, B. platipuda, B. crispa, B. mieroeephala, B. myrioeephala, B. usterii, B. dentata, B. diseolor, B. eliptiea, B. erioelada, B. fastigiata, B. graeilis, B. juneiformis, B. lundii, B.martiana, B. minutiflora, B. multisuleata, B. opuntioides, B. pentziaefolia, B. platypoda, B. serrulata, B. subdentada, B. tarchonanthoides, B.vernonioides, among others, preferably Baceharis dracuneulifoliaD.C.
Particularmente, o presente pedido ainda se apresentacomo extrato bruto de própolis verde brasileira, preparada por abelhas(Apis mellifera africanizadas) a partir do processamento dos ápicesvegetativos de Baccharis dracunculifolia D.C..In particular, the present application is still presented as crude extract of Brazilian green propolis prepared by bees (Apis mellifera africanizada) from the processing of Baccharis dracunculifolia D.C ..
Os óleos essenciais e/ou seus compostos isolados deextratos de Baeeharis spp, do presente pedido, podem ser utilizados emconcentrações de 0,01 a 30% em peso total da composição, sendoposteriormente incorporados nos diferentes sistemas e/ou diferentesvias de administração.The essential oils and / or their compounds isolated from Baeeharis spp extracts, of the present application, may be used in concentrations of from 0.01 to 30% by weight of the total composition, which will later be incorporated into the different delivery systems and / or routes.
Em uma segunda realização, as formulações farmacêuticase/ou cosméticas sugeridas pela presente invenção podem seradministrados por via bucal, oral, tópica, dérmica, transdérmica,ocular, vaginal, retal, uretral e nasal. De forma preferencial, asformulações da presente invenção destinam-se a produtos de usoodontológico e/ou dermo-cosmético, para fins terapêuticos e/ou dehigiene bucal, tais como, enxaguatórios, dentifrícios (pasta, creme, gelou pó), fio dental, vernizes, géis, filmes de rápida absorção, pastilhas,gomas de mascar, porém, não limitados a estes.In a second embodiment, the pharmaceutical and / or cosmetic formulations suggested by the present invention may be administered buccal, oral, topical, dermal, transdermal, ocular, vaginal, rectal, urethral and nasal. Preferably, the formulations of the present invention are intended for dental and / or dermo-cosmetic products for therapeutic and / or oral dehydration purposes, such as mouthwash, dentifrices (paste, cream, frosted powder), dental floss, varnishes. , gels, fast-absorbing films, lozenges, but not limited to chewing gum.
Muitos produtos naturais são insolúveis em água,resultando em baixa dissolução nos veículos de formulações além dapouca biodisponibilidade nos tecidos-alvo, assim, a veiculação dos óleosessenciais e/ou compostos isolados de extrato de Baceharis spp., nasformulações farmacêuticas e/ou cosméticas da presente invençãoocorre através de micro e nanotecnologias.Many natural products are insoluble in water, resulting in low dissolution in formulation vehicles beyond poor bioavailability in target tissues, thus, the delivery of essential oils and / or Baceharis spp. Extract extract, pharmaceutical and / or cosmetic formulations of the present invention. invention occurs through micro and nanotechnologies.
A veiculação dos produtos naturais obtidos de espécies deBaecharis, através de microemulsões, possibilita a melhor solubilizaçãodos princípios ativos, bem como, sua maior preservação contradegradação, oxidação e/ou hidrólise e maior disponibilidade no meiobiológico, seja aumentando a penetração dos princípios ativos embiofilmes, seja aumentando sua absorção pelos tecidos. Além disso, aampla combinação de veículos oleosos e aquosos com surfactantes e co-surfactantes possibilita a obtenção de uma grande variedade deformulações, sejam elas fluidas ou viscosas, em forma líquida, cremosa,pastosa ou gel, adequadas a diversas aplicações farmacêuticas,terapêuticas e cosméticas.The dissemination of natural products obtained from Baecharis species, through microemulsions, allows the best solubilization of the active ingredients, as well as their greater preservation, degradation, oxidation and / or hydrolysis and greater availability in the biological environment, either by increasing the penetration of the embiofilm active principles. increasing its absorption by tissues. In addition, the wide combination of oily and aqueous vehicles with surfactants and co-surfactants enables a wide variety of fluid, creamy, pasty or gel formulas to be obtained, whether fluid or viscous, suitable for various pharmaceutical, therapeutic and cosmetic applications. .
Preferencialmente, a formulação particular da presenteinvenção contém tensoativos, fases oleosas e aquosas, tais como, L-polietilenoglicol-8-caprilato/caprato, P-isoestearato de poligliceril, óleode rícino hidrogenado e etoxilado, monooleato de sorbitano,monolaurato de sorbitano etoxilado, monopalmitato de sorbitanoetoxilado, monoestearato de sorbitano etoxilado, monooleato desorbitano etoxilado, monolaurato de sorbitano, monopalmitato desorbitano, monoestearato de sorbitano, monooleato de sorbitano,glicerol, miristato de isopropila, oleato de etila, triglicérides dos ácidoscáprico / caprílico, polietilenoglicol-6-caprilato/ caprato, poligliceril-6-dioleato e glicerídeos caprilato/caprato, dodecilpoliglicosídeo, carbopol,carboximetilcelulose, hidroxietilcelulose, polietilenoglicol,preferencialmente, óleo essencial de Baccharis spp.Preferably, the particular formulation of the present invention contains surfactants, oily and aqueous phases such as L-polyethylene glycol-8-caprylate / caprate, polyglyceryl P-isostearate, hydrogenated and ethoxylated castor oil, sorbitan monooleate, sorbitan monolaurate ethoxylate sorbitan ethoxylated sorbitan monostearate, ethoxylated sorbitan monostearate, ethoxylated desorbitan monooleate, sorbitan monolaurate, desorbitan monopalmitate, sorbitan monostearate, glycerol, isopropyl myristate, caprylprolyl ethyl acetate / caprylate glyceride, , polyglyceryl-6-dioleate and caprylate / caprate glycerides, dodecylpolyglycoside, carbopol, carboxymethylcellulose, hydroxyethylcellulose, polyethylene glycol, preferably Baccharis spp. essential oil.
Em uma terceira realização, o presente pedido destina-seaos usos das formulações farmacêuticas e/ou cosméticas indicadascomo composições analgésicas, antiinflamatórias, cicatrizantes,antioxidante, antibacteriana, anticariogênica e/ou antineoplásica.In a third embodiment, the present application is for the uses of the pharmaceutical and / or cosmetic formulations indicated as analgesic, anti-inflammatory, scarring, antioxidant, antibacterial, anticaryogenic and / or antineoplastic compositions.
As propriedades antimicrobianas óleos essenciais e/oucompostos isolados de extrato de Baeehans spp, possuem a capacidadede ativar e modular respostas do sistema imunológico celular, além dereduzir a acidez de mucosas, e prevenir e/ou reduzir lesões teciduaismediante agentes irritantes ou indutores.Além disso, seu potencial como antioxidante,antiinflamatório e cicatrizante, também pode ser explorado nasformulações aqui descritas.The antimicrobial properties of essential oils and / or compounds isolated from Baeehans spp extract have the ability to activate and modulate cellular immune system responses, reduce mucosal acidity, and prevent and / or reduce tissue damage by irritating or inducing agents. Its potential as antioxidant, anti-inflammatory and healing can also be explored in the formulations described here.
Os óleos essenciais e/ou compostos de extratos deBaccharis spp. isolados inibem o desenvolvimento de determinadasespécies de bactérias bucais, envolvidas no processo de formação dacárie dental, através de mecanismos bactericidas e não-bactericidasquando utilizadas em formulações odontológicas, anti-sépticas ecosméticas empregadas na higiene bucal.Essential oils and / or extract compounds of Baccharis spp. isolates inhibit the development of certain species of oral bacteria, involved in the process of dental caries formation, through bactericidal and non-bactericidal mechanisms when used in dental formulations, antiseptic used in oral hygiene.
Os mecanismos não-bactericidas dos óleos essenciais e/oucompostos isolados de extrato de Baccharis spp. estão relacionados àinibição da produção bacteriana de ácidos, através da interferênciadireta de seus componentes químicos sobre a atividade de enzimasbacterianas, tais como, aquelas envolvidas no metabolismo de açúcaresfermentáveis (via glicolítica), enzimas de membrana celular bacteriana,envolvidas no sistema transportador de açúcares, e enzimasbacterianas envolvidas na síntese de glucanas de adesão, tambémdenominadas glucosiltransferases, responsáveis pelo acúmulo debactérias nas superfícies dos dentes e formação do biofilme dental.The non-bactericidal mechanisms of essential oils and / or compounds isolated from Baccharis spp. are related to the inhibition of bacterial acid production through the direct interference of their chemical components on the activity of bacterial enzymes, such as those involved in the metabolism of fermentable sugars (glycolytic pathway), bacterial cell membrane enzymes involved in the sugar carrier system, and Bacterial enzymes involved in the synthesis of adhesion glucans, also called glucosyltransferases, responsible for the accumulation of bacteria on the surfaces of the teeth and formation of the dental biofilm.
As propriedades antiinflamatórias e imunomodulatóriasdestes extratos, também apontam grande potencial de aplicação naprevenção e tratamento de periodontites e outros processosinflamatórios da cavidade bucal, de origem bacteriana ou não. Alémdisso, ensaios toxicológicos empregando cultura de células revelaramque o extrato de B. dracuneulifolia possui toxicidade inferior ao dodigluconato de clorohexedina (grupo controle).The antiinflammatory and immunomodulatory properties of these extracts also indicate great potential for application in the prevention and treatment of periodontitis and other oral cavity inflammatory processes, whether bacterial or not. In addition, toxicological assays employing cell culture revealed that B. dracuneulifolia extract has lower toxicity than chlorhexedine dodigluconate (control group).
A atividade antioxidante dos componentes majoritários dopresente extrato, bem como, sua interferência nas vias metabólicasmutagênicas e vias metabólicas bacterianas possivelmente explicam osefeitos antimutagênico e antibacteriano do extrato, respectivamente.The antioxidant activity of the major components of the extract as well as their interference with the metabolic mutagenic pathways and bacterial metabolic pathways possibly explain the antimutagenic and antibacterial effects of the extract, respectively.
ExemplosExamples
Os sistemas micelares emulsionados, microemulsionados enanoemulsinados foram obtidos através da construção de diagramas defase, obtidos de maneira tradicional por titulação lenta de uma série demisturas de óleo/tensoativos com uma fase aquosa, à temperaturaambiente.Emulsified, microemulsified, enanoemulsified micellar systems were obtained by the construction of phase-phase diagrams, traditionally obtained by slowly titrating a series of oil / surfactant mixtures with an aqueous phase at ambient temperature.
As misturas foram tituladas com água purificada, agitadascontinuamente e as regiões de formação de microemulsões,nanoemulsões, emulsões e soluções micelares foram identificadas. Asmicroemulsões foram identificadas como sistemas translúcidos, debaixa viscosidade e isotrópicos.The mixtures were titrated with purified water, stirred continuously and regions of microemulsion, nanoemulsion, emulsion and micellar solution formation were identified. Microemulsions have been identified as translucent, low viscosity and isotropic systems.
Foram construídos 4 diagramas (figura 2) com diferentestipos e misturas de tensoativos, definindo as bases de formulaçõescontendo óleos essenciais e/ou compostos isolados de extratos deBaccharis spp, suas frações cromatográficas e também algumassubstâncias isoladas para uso por diferentes vias de administração.Four diagrams (Figure 2) were constructed with different types and mixtures of surfactants, defining the bases of formulations containing essential oils and / or compounds isolated from Baccharis spp extracts, their chromatographic fractions and also some isolated substances for use by different administration routes.
A análise detalhada dos diagramas de fase mostra que amistura dos componentes das microemulsões em diferentes proporçõespodem gerar vários tipos de agregados nos limites desses diagramas.Assim, no domínio dos agregados polimorfos pode-se detectar aexistência das emulsões, microemulsões, soluções micelares e cristaislíquidos. Nessas várias formas de agregação, microemulsões e cristaislíquidos podem influenciar diferentemente a velocidade de liberação dosfármacos. Como sistemas reservatórios podem alterar os parâmetrosfarmacocinéticos, diminuindo a toxicidade e aumentando a eficáciaclínica de fármacos.Os sistemas que veiculam os extratos de Baccharis,considerando seus tensoativos, fases oleosas e aquosas, são compostospor: Labrasol® (L-polietilenoglicol-8-caprilato/caprato) 2,00 a 89,0%,Plurol® (P-isoestearato de poligliceril) 2,00 a 89,0%, PEG 40 (óleo derícino hidrogenado e etoxilado) 2,00 a 89,0%, Sorbitol (monooleato desorbitano) 0,01 a 89,0%, Glicerol 0,01 a 9,0%, Tween® 20, 40, 60, 80(monolaurato de sorbitano etoxilado, monopalmitato de sorbitanoetoxilado, monoestearato de sorbitano etoxilado, monooleato desorbitano etoxilado) 2,00 a 89,0%, Span® 20, 40, 60, 80 (monolauratode sorbitano, monopalmitato de sorbitano, monoestearato de sorbitano,monooleato de sorbitano) 2,00 a 89,0%, Miristato de Isopropila 0,01 a89,0%, Oleato de Etila 0,01 a 89,0%, Triglicérides dos ácidoscáprico/caprílico 0,01 a 89,0%, Óleo essencial de Baccharis 0,01 a10,0%, Mackaderm MicroExpress® (polietilenoglicol-6-caprilato/caprato,poligliceril-6-dioleato e glicerídeos caprilato/caprato) 2,00 a 80,0%,dodecilpoliglicosídeo 0,01 a 89,0%, Carboximetilcelulse 0,01 a 15,0%,Carbopol® 0,01 a 15,0%, Hidroxietilcelulose 0,01 a 15,0%, PEG 30 a20.000 (polietilenoglicol) 0,01 a 89,0% e água em todas elas, emconcentrações de 0,01 a 95,0%.Detailed analysis of the phase diagrams shows that the mixing of microemulsion components in different proportions can generate various types of aggregates within the boundaries of these diagrams. Thus, in the domain of polymorphic aggregates one can detect the existence of emulsions, microemulsions, micellar solutions and liquid crystals. In these various forms of aggregation, microemulsions and liquid crystals may differently influence the rate of drug release. As reservoir systems can alter pharmacokinetic parameters, reducing toxicity and increasing the clinical efficacy of drugs. Systems that convey Baccharis extracts, considering their surfactants, oily and aqueous phases, are composed by: Labrasol® (L-polyethylene glycol-8-caprylate / caprate) 2.00 to 89.0%, Plurol® (polyglyceryl P-isostearate) 2.00 to 89.0%, PEG 40 (hydrogenated and ethoxylated dericin oil) 2.00 to 89.0%, Sorbitol (monooleate) 0.01 to 89.0%, 0.01 to 9.0% glycerol, Tween® 20, 40, 60, 80 (ethoxylated sorbitan monolaurate, ethoxylated sorbitan monopalmitate, ethoxylated sorbitan monostearate) 2 0.00 to 89.0%, Span® 20, 40, 60, 80 (sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, sorbitan monooleate) 2.00 to 89.0%, Isopropyl myristate 0.01 to 89, 0%, Ethyl Oleate 0.01 to 89.0%, Caprylic / Caprylic Acid Triglycerides 0.01 to 89.0%, Bacc Essential Oil 0.01 to 10.0% haris, Mackaderm MicroExpress® (polyethylene glycol-6-caprylate / caprate, polyglyceryl-6-dioleate and caprylate / caprate glycerides) 2.00 to 80.0%, dodecylpolyglycoside 0.01 to 89.0% Carboxymethylcellulose 0.01 to 15.0%, Carbopol® 0.01 to 15.0%, Hydroxyethylcellulose 0.01 to 15.0%, PEG 30 to 20,000 (polyethylene glycol) 0.01 to 89.0% and water in all of them, concentrations of 0.01 to 95.0%.
A título de exemplo foram construídos diagramas comdiferentes tipos e misturas de tensoativos, contendo extrato brutohidroetanólico de Baccharis dracunculifolia e óleo essencial de Baccharisdracunculifolia.By way of example, diagrams have been constructed with different types and mixtures of surfactants containing crude hydroethanolic extract of Baccharis dracunculifolia and essential oil of Baccharisdracunculifolia.
Diagrama 1Diagram 1
Apresenta uma fase oleosa composta por oleato de etila, afase aquosa por água e a mistura de tensoativo e co-tensoativocomposta por Labrasol® (L-polietilenoglicol-8-caprilato/caprato) ePlurol® (P-isoestearato de poligliceril) na proporção de 3:1.It has an oily phase composed of ethyl oleate, aqueous water aphase and a mixture of surfactant and co-surfactant composed of Labrasol® (L-polyethylene glycol-8-caprylate / caprate) and Plurol® (polyglyceryl P-isostearate) in a proportion of 3 :1.
Diagrama 2Apresenta uma fase oleosa composta por oleato de etila, afase aquosa por água e a mistura de tensoativo e co-tensoativocomposta por PEG 40 (óleo de rícino hidrogenado e etoxilado) e Sorbitolna proporção de 2:1 (PSO).Diagram 2It has an oil phase composed of ethyl oleate, aqueous water-based aphase and the mixture of surfactant and co-surfactant composed of PEG 40 (hydrogenated and ethoxylated castor oil) and Sorbitol in a ratio of 2: 1 (PSO).
Diagrama 3Diagram 3
Apresenta uma fase oleosa composta por miristato deisopropila, a fase aquosa por água e a mistura de tensoativo e co-tensoativo composta por PEG 40 (óleo de rícino hidrogenado e etoxilado)e Sorbitol na proporção de 2:1 (PSM).It has an oily phase composed of deisopropyl myristate, the aqueous phase by water and the surfactant and co-surfactant mixture composed of PEG 40 (hydrogenated and ethoxylated castor oil) and Sorbitol in a ratio of 2: 1 (PSM).
Diagrama 4Diagram 4
Apresenta uma fase oleosa composta por oleato de etila eóleo essencial de Bacchans dracunculifolia, a fase aquosa por água e amistura de tensoativo e co-tensoativo composta por PEG 40 (óleo derícino hidrogenado e etoxilado), Sorbitol e Glicerol na proporção de1:1:1 (PSG).It has an oily phase composed of Bacchans dracunculifolia essential oil and ethyl oleate, the aqueous phase by water and a surfactant and co-surfactant mixture composed of PEG 40 (hydrogenated and ethoxylated dericin oil), Sorbitol and Glycerol in the ratio of 1: 1: 1. (PSG).
Diagrama 5Diagram 5
Apresenta uma fase oleosa composta por oleato de etila eóleo essencial de Baeeharis dracunculifolia, a fase aquosa por Água e amistura de tensoativo e co-tensoativo composta por L-polietilenoglicol-8-caprilato/caprato, P-isoestearato de poligliceril.It presents an oily phase composed of Baeeharis dracunculifolia essential oil and ethyl oleate, the aqueous phase by water and surfactant and co-surfactant mixture consisting of L-polyethylene glycol-8-caprylate / caprate, polyglyceryl P-isostearate.
Diagrama 6Diagram 6
Apresenta uma fase oleosa composta por Triglicerídeos dosácidos cáprico/ caprílico e óleo essencial de Baechans dracunculifolia, afase aquosa por Água e a mistura de tensoativo e co-tensoativocomposta por L-polietilenoglicol-8-caprilato/caprato, P-isoestearato depoligliceril.It has an oily phase composed of capric / caprylic acid triglycerides and Baechans dracunculifolia essential oil, water-based aphasia and the mixture of surfactant and co-surfactant composed of L-polyethylene glycol-8-caprylate / caprate, P-isostearate depolyglyceride.
Diagrama 7Diagram 7
Apresenta uma fase oleosa composta por oleato de etila eóleo essencial de Baccharis dracunculifolia, a fase aquosa por Água e amistura de tensoativo e co-tensoativo composta por monooleato desorbitano e monooleato de sorbitano etoxilado na proporção de 1:2.It has an oily phase composed of Baccharis dracunculifolia essential oil and ethyl oleate, the aqueous phase by water and a surfactant and co-surfactant mixture composed of desorbitan monooleate and ethoxylated sorbitan monooleate in a 1: 2 ratio.
Diagrama 8Diagram 8
Apresenta uma fase oleosa composta por oleato de etila eóleo essencial de Baccharis dracunculifolia, a fase aquosa por Água e amistura de tensoativo e co-tensoativo composta por monooleato desorbitano e monolaurato de sorbitano etoxilado na proporção de 1:3.It has an oily phase composed of Baccharis dracunculifolia essential oil and ethyl oleate, the aqueous phase by water and a surfactant and co-surfactant mixture composed of desorbitan monooleate and ethoxylated sorbitan monolaurate in a 1: 3 ratio.
Posteriormente, foram selecionados sistemas dos 8diagramas a fim de se verificar a influência tanto da (i) porcentagem deóleo como da (ii) mistura de diferentes tensoativos citados na veiculaçãodo extrato e óleo essencial de Baeeharis dracunculifolia. Os diagramasobtidos apontam as quantidades exatas de fase oleosa, tensoativos efase aquosa utilizados na obtenção destes sistemas. O extrato deBaecharis dracunculifolia foi solubilizado na mistura faseoleosa/tensoativo, durante o preparo dos sistemas selecionados.Subsequently, the 8 diagrams systems were selected to verify the influence of both (i) oil percentage and (ii) mixture of different surfactants cited in Baeeharis dracunculifolia extract and essential oil. The diagrams obtained indicate the exact quantities of oil phase, surfactants and aqueous phase used to obtain these systems. Baecharis dracunculifolia extract was solubilized in the oil phase / surfactant mixture during the preparation of the selected systems.
Microscopia de Luz PolarizadaPolarized Light Microscopy
Amostras selecionadas dos diagramas de fases obtidosforam observadas em microscópio de luz polarizada. Foram examinadasamostras que apresentaram transparência (possíveis microemulsões),mas também foram examinadas as amostras translúcidas que porventura foram formadas. Amostras com estas características podem seraltamente birrefringentes e possibilitam a identificação de fase lamelar,por exemplo, que pode também ser utilizada como sistema de liberação.Selected samples of the phase diagrams obtained were observed under a polarized light microscope. Samples that showed transparency (possible microemulsions) were examined, but also translucent samples that may have been formed were examined. Samples with these characteristics can be highly birefringent and allow the identification of lamellar phase, for example, which can also be used as a release system.
EstabilidadeStability
As microemulsões selecionadas foram centrifugadasimediatamente após o preparo a 5000g por 15 minutos, à temperaturaambiente, a fim de se determinar sua estabilidade como um sistemaisotrópico de fase única ou não.The selected microemulsions were centrifuged immediately after preparation at 5000g for 15 minutes at room temperature in order to determine their stability as a single phase or non-single phase isotropic system.
Tamanho das GotículasO tamanho de gotículas dos sistemas selecionados foideterminado com o auxílio de um aparelho Light Scattering Zetasizer4700 (Malvern Instruments, UK).Droplet Size The droplet size of the selected systems was determined with the aid of a Light Scattering Zetasizer4700 apparatus (Malvern Instruments, UK).
ReologiaRheology
Para a determinação do comportamento reológico dasamostras pré-selecionados, foi utilizado um Reômetro Brookfield,modelo DV-III V 3.3 LV, acoplado a um computador com SoftwareRheocalc VI. 1 Brookfield Engineering Laboratories com a utilização despindle SC4-18 e 12 mL de amostra, à 25°C. As medições foramrealizadas em velocidades progressivamente maiores (intervalos de20rpm, de 20 até 200rpm) para a obtenção da curva ascendente e emvelocidades progressivamente menores (intervalo de 20rpm, de 200 a20rpm), no retorno, para obtenção da curva descendente.To determine the rheological behavior of the preselected samples, a Brookfield Rheometer, model DV-III V 3.3 LV, coupled to a computer with SoftwareRheocalc VI, was used. 1 Brookfield Engineering Laboratories using despindle SC4-18 and 12 mL sample at 25 ° C. Measurements were performed at progressively higher speeds (ranges from 20rpm, from 20 to 200rpm) to obtain the upward curve and progressively lower velocities (range from 20rpm, from 200 to 20rpm) at return to obtain the downward curve.
CondutividadeConductivity
A condutividade (em μβ/οπι), dos sistemas selecionados, foideterminada à temperatura ambiente com o auxílio de umcondutivímetro modelo MCA 150 (Tecnopom) a fim de se predizer se osistema em estudo apresenta água ou óleo na fase externa. A adição deágua nas misturas pré-selecionadas de fase oleosa e tensoativos foimonitorada quantitativamente medindo-se a condutividade elétrica. Afase aquosa foi adicionada progressivamente em quantidades de 250μLnas misturas fase oleosa/tensoativos.The conductivity (in μβ / οπι) of the selected systems was determined at room temperature with the aid of a MCA 150 (Tecnopom) conductivity meter to predict whether the system under study has water or oil in the external phase. The addition of water to the preselected oil phase and surfactant mixtures was quantitatively monitored by measuring the electrical conductivity. The aqueous phase was progressively added in amounts of 250μL to the oil phase / surfactant mixtures.
PHPH
Os sistemas selecionados tiveram os valores de pHdeterminados por um pH-metro, modelo 710A (Orion), através de umeletrodo de bulbo fino (modelo 8103, RossM, Orion).The selected systems had pH values determined by a pH-meter, model 710A (Orion), through a thin bulb electrode (model 8103, RossM, Orion).
Índice de RefraçãoRefractive index
O índice de refração dos sistemas selecionados foideterminado através de refratômetro digital ABBE Mark II, por adiçãode uma alíquota de 50μ1-, da amostra na câmara do mesmo, seguido deleitura manual.The refractive index of the selected systems was determined by ABBE Mark II digital refractometer by the addition of a 50μ1- aliquot of the sample in the chamber, followed by manual readout.
Determinação do Perfil do Filtrado, por Cromatografia Líquida deDetermination of Filtrate Profile by Liquid Chromatography of
Alta Eficiência (CLAE)High Efficiency (HPLC)
A cromatografia líquida de alta eficiência (CLAE) foiutilizada para análise do perfil do extrato bruto etanólico de Baccharisdracunculifolia e do resíduo filtrado de alguns sistemas selecionados.High performance liquid chromatography (HPLC) was used to analyze the profile of the crude ethanolic extract of Baccharisdracunculifolia and the filtered residue of some selected systems.
Para as análises em cromatografia líquida de alta eficiência foramempregados solventes de grau cromatográfíco e a água empregada napreparação das soluções foi purificada em sistemas de filtro MILLI-Q-PLUS da MILLIPORE. Todos os solventes e soluções empregados comofases móveis em CLAE foram filtrados em membrana de nitrato decelulose. As análises foram realizadas em cromatógrafo de fase líquidade alta eficiência, equipado com controlador SCL-lOAfp, com trêsbombas LC-10AD, detector de arranjo de diodos modelo SPD - MlOAyp,e sistema controlador computadorizado com software Shimadzu Class-VP versão 5.02. Também foi utilizada uma coluna cromatográficaanalítica de fase reversa Shim-pack CLC - ODS (M), Shimadzu, 4,6 mmχ 250 mm, diâmetro de partícula 5 pm e diâmetro de poro 100Â,protegida por pré-coluna C18 SGE.For the analyzes in high performance liquid chromatography, chromatographic grade solvents were employed and the water used in the preparation of the solutions was purified in MILLIPORE MILLI-Q-PLUS filter systems. All solvents and solutions employed as HPLC mobile phases were filtered through a cellulose nitrate membrane. The analyzes were performed in a high performance liquid chromatography phase equipped with SCL-10Afp controller, with three LC-10AD pumps, SPD - MlOAyp diode array detector, and Shimadzu Class-VP software version 5.02. A Shim-pack CLC - ODS (M), Shimadzu, 4.6 mmχ 250 mm, 5 µm particle diameter and 100 µ pore diameter, protected by C18 SGE pre-column, was also used.
DensidadeDensity
A densidade, relação entre massa e volume, foi determinadapela densidade relativa, que é a relação entre a densidade absoluta deuma substância e a densidade absoluta de outra substânciaestabelecida como padrão. Para este caso, a substância padrão foi águapurificada. A densidade relativa dos sistemas selecionados foideterminada à temperatura de 20°C, pelo método tradicional dopicnômetro. A densidade da amostra (sistema selecionado) foi calculadaatravés de uma equação, onde: d = densidade; Mo = massa dopicnômetro vazio; Mi = massa do picnômetro com água purificada a20°C; e M2 = massa do picnômetro com a amostra a 20°C.Density, the ratio of mass to volume, was determined by the relative density, which is the ratio between the absolute density of one substance and the absolute density of another substance as standard. For this case, the standard substance was water purified. The relative density of the selected systems was determined at a temperature of 20 ° C by the traditional dopicnometer method. Sample density (selected system) was calculated using an equation, where: d = density; Mo = empty dopicnometer mass; Mi = pycnometer mass with purified water at 20 ° C; and M2 = pycnometer mass with the sample at 20 ° C.
Foram selecionados sistemas dos diagramas obtidos a fimde se verificar a influência tanto da (i) porcentagem de óleo como da (ii)mistura de diferentes tensoativos na veiculação dos extratos deBaccharis. Para o enxaguatório bucal, preferencialmente, foramescolhidos os sistemas com maior conteúdo aquoso e com menorviscosidade.Systems were selected from the diagrams obtained in order to verify the influence of both (i) percentage of oil and (ii) mixture of different surfactants on Baccharis extracts. For the mouthwash, preferably, the systems with the highest aqueous content and the lowest viscosity were chosen.
Tabela 1Table 1
<table>table see original document page 21</column></row><table><table> table see original document page 21 </column> </row> <table>
Claims (16)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| BRPI0900802A BRPI0900802B8 (en) | 2009-03-12 | 2009-03-12 | pharmaceutical and/or cosmetic formulations containing essential oils and compounds isolated from extracts of baccharis spp. |
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| Application Number | Priority Date | Filing Date | Title |
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| BRPI0900802A BRPI0900802B8 (en) | 2009-03-12 | 2009-03-12 | pharmaceutical and/or cosmetic formulations containing essential oils and compounds isolated from extracts of baccharis spp. |
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| Publication Number | Publication Date |
|---|---|
| BRPI0900802A2 true BRPI0900802A2 (en) | 2010-11-09 |
| BRPI0900802B1 BRPI0900802B1 (en) | 2020-03-24 |
| BRPI0900802B8 BRPI0900802B8 (en) | 2021-05-25 |
Family
ID=43064045
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0900802A BRPI0900802B8 (en) | 2009-03-12 | 2009-03-12 | pharmaceutical and/or cosmetic formulations containing essential oils and compounds isolated from extracts of baccharis spp. |
Country Status (1)
| Country | Link |
|---|---|
| BR (1) | BRPI0900802B8 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2022082277A1 (en) * | 2020-10-19 | 2022-04-28 | BATOCCHIO, Ana Lúcia Torrez | Propolis-based natural composition and preparation method |
| US11998572B2 (en) | 2021-06-29 | 2024-06-04 | Imam Abdulrahman Bin Faisal University | Method for treating nociceptive pain and burns with brazilian green propolis alcohol extract |
-
2009
- 2009-03-12 BR BRPI0900802A patent/BRPI0900802B8/en active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0900802B8 (en) | 2021-05-25 |
| BRPI0900802B1 (en) | 2020-03-24 |
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