RESUMO
The goal of this work was the development of natural polymeric microcapsules for antimicrobial drug delivery - triclosan loaded alginate and chitosan-based microcapsules for potential coating applications in substrates such as textiles or plastics. Microcapsules containing 2.5% (w/w) or 3% (w/w) triclosan in both core and matrix were synthesized and evaluated by Fourier-transform infrared spectroscopy, scanning electron microscopy, confocal microscopy, differential scanning calorimetry, thermogravimetry, and antimicrobial activity. The microcapsules produced featured spherical and mostly irregularly-shaped surfaces composed by an alginate core in a chitosan outer matrix, as revealed by confocal microscopy, and antimicrobial activity against S. aureus and E. coli with inhibition halos up to 60 mm and 25 mm respectively, granted by a triclosan loading of 61.66%. The thermal analysis suggested that the polymers protected the active substance from temperature-induced degradation. In conclusion, these microcapsules may be applied toward antimicrobial functionalization of plastics, textiles and other materials.
Assuntos
Alginatos/química , Anti-Infecciosos/química , Quitosana , Triclosan , Cápsulas , Escherichia coli , Espectroscopia de Infravermelho com Transformada de Fourier , Staphylococcus aureusRESUMO
Mosquito-borne diseases such as dengue, malaria, yellow fever, chikungunya and Zika virus affect millions of people worldwide each year. Vector control and personal protection are very important to minimize the spread of diseases, and the use of repellent is an economic practice to prevent them. The application of repellent, which acts on the skin to form a vapor layer with a repellent odor to mosquitos, is recommended as an economic prevention and practice. The natural botanical product Citronella is an effective mosquito repellent due to the high concentrations of active chemical constituents present, notably terpenic alcohols. However, citronella tends to evaporate quickly from the skin surface, resulting in a rapid loss of activity. Strategies to increase repellency time, while at the same time minimizing toxicity, are major focuses of research and development in natural repellent products. Here we highlight the role of extended-release systems (ERS) of citronella oil in this approach.
Assuntos
Produtos Biológicos , Repelentes de Insetos , Malária , Infecção por Zika virus , Zika virus , Animais , Humanos , Repelentes de Insetos/farmacologia , Composição de Medicamentos , TerpenosRESUMO
The skin microbiome is crucial in maintaining skin health, and its disruption is associated with various skin diseases. Prebiotics are non-digestible fibers and compounds found in certain foods that promote the activity and growth of beneficial bacteria in the gut or skin. On the other hand, live microorganisms, known as probiotics, benefit in sustaining healthy conditions when consumed in reasonable quantities. They differ from postbiotics, which are by-product compounds from bacteria that release the same effects as their parent bacteria. The human skin microbiome is vital when it comes to maintaining skin health and preventing a variety of dermatological conditions. This review explores novel strategies that use microbiome-targeted treatments to maintain and enhance overall skin health while managing various skin disorders. It is important to understand the dynamic relationship between these beneficial microorganisms and the diverse microbial communities present on the skin to create effective strategies for using probiotics on the skin. This understanding can help optimize formulations and treatment regimens for improved outcomes in skincare, particularly in developing solutions for various skin problems.
RESUMO
Mosquito-borne diseases affect millions of people worldwide each year, and the use of a topically applied insect repellent is an economically viable preventative health practice. The general objective of this work was to encapsulate citronella oil (CO) in a nanostructured lipid carrier (NLC) to formulate a topical repellent with a long duration of efficacy on the skin and a good safety profile based on minimizing skin penetration. In the studied CO, the main chemical constituents of geraniol, citronellal, and citronellol were identified and subsequently used as markers for the in vitro skin permeation testing (IVPT). An optimal NLC encapsulating CO formulation was developed and had an average particle size of 350 nm. The NLC was then formulated in combination with CO at ratios of 2:1, 1:1, and 1:2 CO:NLC-CO as oil-in-water (O/W) emulsions and compared to CO in the same O/W emulsion base (all at 10% CO in the final O/W topical formulation). The markers geraniol, citronellol, and citronellal were detected in all samples tested F1 (10% CO in O/W emulsion) and F3 (10% CO/NLC-CO 1:1 in O/W emulsion). Even the percentages of F3 markers were higher than F1. The recovery of the percentage balance (based on the total remaining on the skin surface, on the skin, and penetrated through the skin to the receptor) of geraniol, citronellol, and citronellal markers for F1 and F3 was 7.70% and 11.96%; 25.51% and 31.89%; and 5.09% and 4.40%, respectively. The nanoparticle lipid solid forms a repellent reservoir on the skin surface, releasing the active ingredients slowly through volatilization, extending the repellent action, and reducing permeation through the skin. It is possible to assume that the remaining 92.30% and 88.03%; 74.49% and 68.11%; and 94.10% and 95.60% of geraniol, citronellol, and citronellal markers of F1 and F3, respectively, were lost to evaporation. In the in vivo efficacy test carried out with the Aedes aegypti mosquito, F3 was the optimal formulation, providing the greatest repellent action compared to free oil in O/W emulsion. Thermal analysis showed that the NLC-CO raised the boiling point of the encapsulated CO compared to the free oil, suggesting that the controlled release of the CO was a possible mechanism for its prolonged effect. We concluded that the nanocarriers developed with CO were stable and provided improved mosquito-repellent efficacy with minimal skin penetration of the CO actives over 24 h. Indeed, regardless of whether the CO was applied as free oil, a 1:1 mixture of CO (pure/free oil) or NLC-CO applied in an O/W emulsion can be considered safe for topical application due to minimal skin penetration.
RESUMO
OBJECTIVE: This study aimed to develop a holobiont tablet with rapid dispersibility to provide regulation of the microbiota, virucidal activity, and skin barrier protection. METHODS: A 23 factorial experiment was planned to define the best formulation for the development of the base tablet, using average weight, hardness, dimensions, swelling rate, and disintegration time as parameters to be analyzed. To produce holobiont tablets, the chosen base formulation was fabricated by direct compression of prebiotics, postbiotics, and excipients. The tablets also incorporated solid lipid nanoparticles containing postbiotics that were obtained by high-pressure homogenization and freeze-drying. The in vitro virucidal activity against alpha-coronavirus particles (CCoV-VR809) was determined in VERO cell culture. In vitro analysis, using monolayer cells and human equivalent skin, was performed by rRTq-PCR to determine the expression of interleukins 1, 6, 8, and 17, aquaporin-3, involucrin, filaggrin, FoxO3, and SIRT-1. Antioxidant activity and collagen-1 synthesis were also performed in fibroblast cells. Metagenomic analysis of the skin microbiome was determined in vivo before and after application of the holobiont tablet, during one week of continuous use, and compared to the use of alcohol gel. Samples were analyzed by sequencing the V3-V4 region of the 16S rRNA gene. RESULTS: A handrub tablet with rapid dispersibility was developed for topical use and rinse off. After being defined as safe, the virucidal activity was found to be equal to or greater than that of 70% alcohol, with a reduction in interleukins and maintenance or improvement of skin barrier gene markers, in addition to the reestablishment of the skin microbiota after use. CONCLUSIONS: The holobiont tablets were able to improve the genetic markers related to the skin barrier and also its microbiota, thereby being more favorable for use as a hand sanitizer than 70% alcohol.
RESUMO
BACKGROUND: Dipteryx alata Vogel popularly known as "baru" is an important commercial leguminous tree species from the Brazilian Cerrado, which possess medicinal properties, besides its fruits consumption by animals and humans. The use of the "naturally occurring plants" as herbal remedies and foods mainly from leaves, seeds, flowers and roots of plants or extracts require precautions before ensuring these are safe and efficacious. The objective of this study was to evaluate the safety of D. alata barks extract. METHODS: Vegetal drugs of D. alata barks were submitted to quality control assays and further to the safety assays under 1) in vitro parameter by Salmonella (Ames) mutagenicity, and 2) in vivo parameter on the pregnancy of rats. RESULTS: The extract was non-mutagenic to any of the assessed strains TA97a, TA98, TA100 and TA102 even after metabolic activation (+S9). All in vivo parameters (reproductive ability evaluation, physical development of rat offsprings, and neurobehavioral development assays) showed no changes related to control group. CONCLUSION: D. alata barks extract is neither mutagenic by the Ames test nor toxic in the pregnancy of rats, with no physical-neurobehavioral consequences on the rat offsprings development.
Assuntos
Dipteryx/efeitos adversos , Extratos Vegetais/efeitos adversos , Animais , Animais Recém-Nascidos , Feminino , Humanos , Masculino , Mutagênicos , Casca de Planta , Gravidez/efeitos dos fármacos , Ratos , Ratos Wistar , Reprodução/efeitos dos fármacos , Salmonella/efeitos dos fármacosRESUMO
Even though the synthetic preservatives may offer a high antimicrobial efficacy, they are commonly related to adverse reactions and regarded as having potentially harmful effects caused by chronic consumption. The development of natural preservatives provides a way of reducing the amount of synthetic preservatives normally used in pharmaceutical and cosmetic preparations. In addition, these agents have less toxic effects and represent a possible natural and safer alternative of the preservatives. The purpose of this research was to evaluate the Rubus rosaefolius Smith extract efficiency as a natural preservative in base formulations. Of the extract, 0.2% (w/w) was assayed for its effectiveness of antimicrobial protection in two different base formulations (emulsion and gel). The microbial challenge test was performed following the standard procedures proposed by The United States Pharmacopoeia 33nd, European Pharmacopoeia 6th, Japanese Pharmacopoeia 15th, and the Cosmetics, Toiletries, and Fragrance Association using standardized microorganisms. The results demonstrated that R. rosaefolius extract at the studied concentration reduced the bacterial inocula, satisfying the criterion in all formulations, even though it was not able to present an effective preservative behavior against fungi. Thus, the investigation of new natural substances with preservative properties that could be applied in pharmaceutical and cosmetic products is relevant due to the possibility of substituting or decreasing the concentration of synthetic preservatives, providing a way for the development of safer formulas for the use of consumers.
Assuntos
Produtos Biológicos/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Conservantes Farmacêuticos/química , Rosaceae , Administração Tópica , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Produtos Biológicos/administração & dosagem , Produtos Biológicos/isolamento & purificação , Química Farmacêutica , Cosméticos/administração & dosagem , Cosméticos/química , Cosméticos/isolamento & purificação , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana/métodos , Farmacopeias como Assunto , Extratos Vegetais/administração & dosagem , Folhas de Planta/química , Conservantes Farmacêuticos/administração & dosagem , Conservantes Farmacêuticos/isolamento & purificação , Estados UnidosRESUMO
Extracts from Dipteryx alata bark obtained with different solvents (hexane, dichloromethane, ethyl acetate and methanol) were mixed in vitro with Bothrops jararacussu (Bjssu, 40 µg/mL) and Crotalus durissus terrificus (Cdt, 15 µg/mL) snake venoms, and applied to a mouse phrenic nerve-diaphragm preparation to evaluate the possible neutralization of venom effects. Cdt venom neurotoxic effect was not inhibited by any of the extracts, while the neurotoxic and myotoxic actions of Bjssu venom were decreased by the methanolic extract. This inhibition appears to be augmented by tannins. Dichloromethane bark extract inhibited ~40% of Bjssu venom effects and delayed blockade induced by Cdt. The methodology used to determine which extract was active allows inferring that: (i) phenolic acids and flavonoids contained in the methanolic extract plus tannins were responsible mostly for neutralization of Bjssu effects; (ii) terpenoids from the dichloromethane extract may participate in the anti-Cdt and anti-Bjssu venom effects; (iii) a given extract could not inhibit venoms from different species even if those belong to the same family, so it is improper to generalize a certain plant as antiophidian; (iv) different polarity extracts do not present the same inhibitory capability, thus demonstrating the need for characterizing both venom pharmacology and the phytochemistry of medicinal plant compounds.
Assuntos
Antivenenos/isolamento & purificação , Antivenenos/farmacologia , Dipteryx/química , Nervo Frênico/efeitos dos fármacos , Animais , Bothrops , Crotalus , Metanol , Cloreto de Metileno , Camundongos , Casca de Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Especificidade da Espécie , Peçonhas/toxicidadeRESUMO
In this study, we proposed the use of the biopolymers silk fibroin, chitosan and alginate, which are recognized for their biocompatibility and biodegradability, for the preparation of multilayer membranes aiming at high performance wound dressings with controlled drug delivery. The rationale was to combine in one material the mechanical properties of fibroin, the antimicrobial action of chitosan and the ideal exudate absorption of alginate, reaching a synergic effect of each biopolymer, without losing their individual intrinsic properties. The membranes were prepared by casting and diclofenac sodium was incorporated as model drug into the chitosan solution before the solvent evaporation, being retained in the middle layer of the membrane. Morphological, thermal, mechanical, solubility and barrier properties of the membranes were evaluated, as well as cytotoxicity and microbiological permeation. Results show that the incorporation of the drug did not affect mechanical and barrier properties, as well as microbiological permeation. Drug release was evaluated in vitro using simulated solution of wound exudate at 37 °C and diclofenac sodium was released from the multilayer membrane in 7 h, in which Fickian diffusion was the main mechanism associated. The results show the potential application of the biopolymer multilayer membranes as high-performance wound dressings.
Assuntos
Alginatos/química , Quitosana/química , Preparações de Ação Retardada/química , Fibroínas/química , Membranas/química , Seda/química , Bandagens , Materiais Biocompatíveis/química , Biopolímeros/química , Preparações de Ação Retardada/farmacologia , Liberação Controlada de Fármacos/efeitos dos fármacos , Cicatrização/efeitos dos fármacosRESUMO
Biopolymeric films can be used as dressings for the treatment of skin burns and other chronic wounds. The healing properties of these films may be enhanced by the addition of Copaiba oil (Copaifera L.) which properties have already been well-described. The aim of this study was to evaluate the addition of Copaiba oil in chitosan films prepared by casting solvent evaporation technique using chitosan solution (2% or 1% wt/wt) and Copaiba oil (0.1 or 1.0% wt/wt) at different concentrations. Films were characterized by color analysis, scanning electron microscopy, mechanical properties, thermal analysis, and fluid handling capacity. The developed films demonstrated potential for wound dressing, translated by the fluid handling capacity similar to that of commercial dressings. While no surfactant was present in the formulation, the droplets of Copaiba oil were well-dispersed and homogeneously distributed in the chitosan matrix even after drying. The thermal analysis translated the occurrence of interactions between the oil and chitosan.
Assuntos
Quitosana/química , Preparações de Plantas/administração & dosagem , Solventes/química , Cicatrização/efeitos dos fármacos , Bandagens , Química Farmacêutica/métodos , Portadores de Fármacos/química , Microscopia Eletrônica de Varredura , Preparações de Plantas/químicaRESUMO
A novel bilayer film of chitosan and konjac glucomannan were prepared by the two-step casting technique. Blend films were also prepared to investigate the interactions between the two polymers in the interfacial region of the bilayer structure. Scanning electron microscopy, Fourier transform infrared spectroscopy, and X-ray diffraction analysis showed that, unlike in the blends, the physicochemical properties of each biopolymer were preserved in the bilayer film. Differential scanning calorimetry and thermogravimetric analysis also indicated a good thermostability and miscibility for both polymers, probably due to strong hydrogen bonds between their polymer chains. Biological, mechanical and water vapor transmission tests showed a high biocompatibility, low cytotoxicity, and suitable mechanical and barrier properties of the bilayer films for wound dressing applications.
Assuntos
Bandagens , Quitosana/síntese química , Mananas/síntese química , Plantas , Candida albicans/efeitos dos fármacos , Candida albicans/fisiologia , Quitosana/farmacologia , Cromatografia em Gel/métodos , Avaliação Pré-Clínica de Medicamentos/métodos , Escherichia coli/efeitos dos fármacos , Escherichia coli/fisiologia , Mananas/farmacologia , Resistência à Tração/efeitos dos fármacos , Resistência à Tração/fisiologia , Difração de Raios X/métodosRESUMO
Abstract In this study, we investigated the influence of the olfactive stimulus on visual attention. Two groups of 30 subjects participated in two experiments. Both experiments presented two arrays of fruits stimulus intercalated by an olfactive intervention. The stimulus was received in the form of images by the first group and in the form of words by the second group. An eye-tracking device monitored the timekeeping of visual attention dispensed in each stimulus. The results showed that olfactive priming influenced visual attention in both cases but with a greater degree in the images stimulus group. This study shows for the first time that image information is more susceptible to priming olfactive information than wording information. This effect may be associated with the formation of mental images in working memory, aroused by fragrances.
RESUMO
The interaction of surfactants sodium dodecyl sulfate (SDS), cetyl trimethyl ammonium chloride (CTAC) and lauryl alcohol ethoxylated (12 mol ethylene oxide) (LAE-12OE) was evaluated on the stratum corneum (SC) of shed snake skins from Bothrops jararaca, used as model membrane, and thermal characterized by differential scanning calorimetry (DSC). Surfactant solutions were employed above of the critical micellar concentration (CMC) with treatment time of 8h. The SDS interaction with the SC model membrane has increased the characteristic transition temperature of 130 degrees C in approximately 10 degrees C for the water loss and keratin denaturation, indicating an augmentation of the water content. Samples treated with CTAC have a decrease of the water loss temperature, while, for the LAE-12OE treated samples, changes on the transition temperature have not been observed.
Assuntos
Bothrops , Epiderme/química , Tensoativos/química , Animais , Varredura Diferencial de Calorimetria , Cetrimônio , Compostos de Cetrimônio/química , Dodecanol/química , Técnicas In Vitro , Dodecilsulfato de Sódio/químicaRESUMO
This research employed FT-Raman and PAS-FTIR spectroscopic techniques to evaluate the interaction of cetyl trimethyl ammonium chloride (CTAC), a cationic surfactant, on the stratum corneum (SC) of shed snake skins from Bothrops jararaca, used as model membranes. Surfactant aqueous solutions (50.0 and 0.78 gl(-1)) with neutral pH were applied on the samples with intervals of 4, 8 (whole SC) and 12h (SC tape-stripped). Samples presented modifications of the topography for all conditions of the assays and the monomers of the surfactant, instead of the micelles, seemed to interact with the keratin. The SC model membranes treated with CTAC have had an augment of water content (except for whole SC treated for 8h) indicated by the expansion of the band 3600-3300 cm(-1), mainly for the tape-stripped samples after 12h treatment. Concentration appeared to be an important factor related to an increase of the tissue hydration.
Assuntos
Compostos de Cetrimônio/química , Epiderme/química , Membranas/química , Tensoativos/química , Animais , Bothrops , Cetrimônio , Compostos de Cetrimônio/farmacologia , Epiderme/efeitos dos fármacos , Membranas/efeitos dos fármacos , Modelos Biológicos , Soluções/química , Espectroscopia de Infravermelho com Transformada de Fourier , Análise Espectral Raman , Tensoativos/farmacologia , Água/químicaRESUMO
Urea's thermal instability and burning on sensitive skin can cause problems for cosmetic formulations. To overcome these drawbacks, urea was incorporated into ordered mesoporous silica (SBA-15). SBA-15 was synthesized using tetraethyl orthosilicate and Pluronic® P123 in an acid medium. Urea (20 wt.%) was incorporated into calcined SBA-15 by the incipient wetness impregnation method. Several techniques were used to characterize the samples. Skin hydration and transepidermal water loss were measured using Corneometer® CM 825 PC and Tewameter® 300 TM. Results showed that the structural properties of SBA-15Urea were similar to pure SBA-15, indicating that SBA-15 remained structured even after urea incorporation. Nitrogen physisorption data showed the volume and surface area of the pores in SBA-15Urea were much lower than those in SBA-15, demonstrating that urea was deposited inside the mesopores. In vivo moisturization studies revealed that SBA-15Urea was not able to reduce transepidermal water loss compared to the other products and control, while forming a non-occlusive surface film on the skin. We conclude that incorporation of urea in the pores of the inorganic SBA-15 matrix is a promising approach to enhancing its stability and providing a prolonged moisturizing effect.
Assuntos
Ureia/análise , Dióxido de Silício/administração & dosagem , Pele/efeitos dos fármacos , Hidratação/efeitos adversosRESUMO
Scientific assessment of harmful interactions of chemicals over the entire reproductive cycle are divided into three segments based on the period: from premating and mating to implantation (I), from implantation to major organogenesis (II), and late pregnancy and postnatal development (III). We combined the segments I and II to assess Plathymenia reticulata aqueous extract safety. In order to investigate reproductive toxicity (segment I), pregnant rats received orally 0.5 or 1.0 g/kg of extract, daily, during 18 days. These concentrations were determined by a preliminary in vitro LD50 test in CHO-k1 cells. A control group received deionized water. The offspring was removed at the 19th day, by caesarean, and a teratology study (segment II) was carried out. The corpora lutea, implants, resorptions, live, and dead fetuses were then counted. Placenta and fetuses were weighted. External and visceral morphology were provided by the fixation of fetuses in Bouin, whereas skeletal analysis was carried out on the diaphanizated ones. The increase in the weights of placenta and fetuses was the only abnormality observed. Since there was no sign of alteration on reproduction parameters at our experimental conditions, we conclude that P. reticulata aqueous extract is safe at 0.5 to 1.0 g/kg and is not considered teratogenic.
Assuntos
Feto/efeitos dos fármacos , Organogênese/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Animais , Relação Dose-Resposta a Droga , Fabaceae/química , Feminino , Humanos , Extratos Vegetais/química , Gravidez , Ratos , Teratogênicos/química , Teratogênicos/farmacologia , Água/químicaRESUMO
ABSTRACT Aiming to alter and/or improve permeation of active compounds in the skin, many strategies have been developed, including biophysical methods. One of the physical absorption techniques, currently known as Cryo Laser Phoresis (CLP), consists of an apparatus that emits radiation on polar or nonpolar molecules of the active substance, resulting in faster penetration when in comparison to the standard topical application. The goal of this work was to evaluate the efficacy of a method that proposes to increase cutaneous permeation of diclofenac sodium by using CLP technique. The influence on permeation was evaluated ex vivo, using Franz cell and human skin obtained from cosmetic surgery. The results were evaluated using statistical methods and data exploratory analysis: clusters, k-means and Principal Component Analysis. The results showed a larger increase in the concentration of diclofenac sodium in the dermis with the use of laser. In all samples (with or without laser application) it was observed that skin surface showed an amount of diclofenac sodium and that there was no active passage to the receptor liquid, suggesting that diclofenac sodium was not absorbed. These results indicate that CLP, when used under the conditions described in this study, is able to increase diclofenac sodium penetration and its retention into deeper layers.
RESUMO No sentido de alterar e/ou melhorar a penetração de substâncias na pele, diversas estratégias têm sido desenvolvidas, variando desde a aplicação de novos veículos e ativos encapsulados, até equipamentos que atuam por métodos biofísicos. Uma das técnicas de absorção física, atualmente conhecida como Crio Laser Forese (CLF), consiste em um aparato que emite radiação sobre moléculas polares ou apolares da substância ativa, tornando sua penetração mais rápida, se comparada à administração tópica comum. O objetivo deste trabalho foi avaliar a eficácia de um método que propõe aumentar a permeação cutânea do diclofenaco de sódio incorporado a um gel, por meio do uso da CLF. A influência sobre a permeação foi avaliada ex vivo, utilizando célula de Franz e pele humana obtida de cirurgia plástica. Os resultados foram balizados mediante aplicação de métodos estatísticos e análise exploratória de dados: clusters, k-means e Análise por Componentes Principais. Os resultados demonstraram aumento na concentração do diclofenaco de sódio na derme com o uso do laser. Em todas as amostras (com ou sem aplicação de laser), observou-se, uma quantidade de diclofenaco de sódio na superfície da pele e que não houve passagem de ativo para o líquido do receptor, sugerindo que o diclofenaco de sódio não foi absorvido. Estes resultados indicam que CLF usada sob as condições descritas neste estudo é capaz de aumentar a penetração do diclofenaco de sódio e sua retenção em camadas mais profundas da pele.
Assuntos
Diclofenaco/farmacocinética , Lasers , Pele/efeitos dos fármacos , Fármacos Dermatológicos/farmacocinéticaRESUMO
Papain is an enzyme used in topical formulations as a proteolytic debriding agent for the treatment of open, extensive wounds and burnings. It is also employed as an enhancer for cutaneous permeation of active compounds, chemical peeling and as a progressive depilatory agent. The stability of formulations containing enzymes is not easy. In this research, papain was modified with polyethylene glycol in order to increase the stability of the formulations. The comparative Normal Stability Testing of the topical formulations containing unmodified and modified papain showed that the modified variety presented with a differentiated profile under the adopted temperature conditions (5.0 ± 1.0 °C; 22.0 ± 2.0 °C; 40.0 ± 2.0 °C). The most suitable condition for non-modified papain were 5.0 ± 1.0 °C and, for modified papain, they were 22.0 ± 2.0 °C. These results confirmed the higher stability of modified papain compared to free papain, as well as its potential to be applied in topical formulations.
A papaína é uma enzima utilizada em formulações tópicas como agente proteolítico debridante no tratamento de lesões abertas de grande extensão e queimaduras. É, também, empregada na pele íntegra como agente promotor da permeação cutânea de princípios ativos, peeling químico e como agente depilatório progressivo. A estabilidade de formulações contendo enzimas não é facilmente alcançada. No presente trabalho realizou-se a modificação da enzima com polietilenoglicol, visando maior estabilidade das formulações. A realização do Teste Estabilidade Normal comparativo entre as formulações contendo as formas da enzima não modificada e modificada demonstrou que a última apresentou um perfil de estabilidade diferenciado, nas diferentes condições (5,0 ± 1,0 °C; 22,0 ± 2,0 °C; 40,0 ± 2,0 °C). A condição de 5,0 ± 1,0 °C foi a mais adequada para a formulação contendo papaína não modificada enquanto a 22,0 ± 2,0 °C foi indicada para aquela contendo a forma modificada. Estes resultados confirmaram o aumento da estabilidade da papaína modificada comparada com a livre e seu potencial de aplicação em formulações de uso tópico.
Assuntos
Estudo Comparativo , Papaína/análise , Química Farmacêutica , Polietilenoglicóis/farmacocinéticaRESUMO
The purpose of this research was to determine the potential of papain and pequi oil as penetration enhancers for diclofenac sodium (DS) across human skin in vitro. The permeation studies were conducted with vertical diffusion cells. The enhancers were associated or not in gels in different concentrations. In vitro studies reveled that papain 0.2 percent (w/v) presented an elevated enhancer property for diclofenac sodium (J = 0.3369 mg/cm²x h). Pequi oil 10 percent (w/v) generated a reduced flux value (J = 0.1848 mg/cm²x h) and a combination of both enhancers presented a medium value of J = 0.2187 mg/cm²x h. Papain was found to be better enhancer than pequi oil.
O objetivo desta pesquisa foi determinar in vitro o potencial da papaína e do óleo de pequi como promotores de penetração cutânea para o diclofenaco de sódio (DS) através de pele humana. Os estudos de penetração foram conduzidos em células de difusão vertical. Os promotores foram associados ou não em géis em concentrações distintas. A avaliação in vitro revelou que a papaína 0,2 por cento p/p apresentou propriedade promotora maior para o diclofenaco de sódio (J = 0,3369 mg/cm²x h). O óleo de pequi 10,0 por cento p/v promoveu redução do fluxo (J = 0,1848 mg/cm²x h) e a combinação de ambos os promotores apresentou valor mediano de fluxo de J = 0,2187 mg/cm²x h. A partir dos resultados, verificou-se que a papaína exerceu ação promotora de penetração cutânea melhor que o óleo de pequi.