Green tea glycolic extract-loaded liquid crystal systems: development, characterization and microbiological control

ABSTRACT Liquid crystal systems (LCSs) have interesting cosmetic applications because of their ability to increase the therapeutic efficiency and solubility of active ingredients. The aim of the present research was to develop green tea glycolic extract-loaded LCSs, to characterize and to perform microbiological control. The ternary phase diagram was constructed using polysorbate 20, silicone glycol copolymer (SGC) - DC 193(r), and distilled water with 1.5% glycolic green tea extract. The systems were characterized by polarized light microscopy. Formulations selected were characterized as transparent viscous systems and transparent liquid system indicated mesophases lamellar structure. The results of the microbiological analysis of mesophilic aerobic microorganisms (bacteria and fungi) revealed that the above formulation showed a biologic load <10 CFU/mL in all samples. In conclusion, liquid crystalline systems that have presented formation of a lamellar mesophases were developed. Furthermore, the formulation and products tested presented the adequate microbiological quality in accordance with official recommendations

Tretinoin-based formulations - influence of concentration and vehicles on skin penetration

Tretinoin is used in the management of acne and it is part of a gold standard treatment for photoaging. It has also been reported as an agent for superficial chemical peeling in highly concentrated formulations with few considerations about skin penetration. The aim of this study was to evaluate the influence of drug concentration and vehicles currently used on skin penetration of tretinoin. In vitro permeation tests were carried out using Franz diffusion cells fitted with porcine ear skin and 10% aqueous methanol in the receptor compartment. Formulations studied, cream or hydroalcoholic dispersion, containing 0.25%, 1% and 5% of tretinoin were placed in the donor compartment for six hours. Tretinoin concentration in skin layers was measured by high performance liquid chromatography. The largest amount of tretinoin from both vehicles was detected in stratum corneum with significant differences among the three concentrations. The hydroalcoholic dispersion was the best vehicle. Significant amounts of tretinoin were found even in deep layers of epidermis. The formulation with 0.25% tretinoin showed better results when considered the amount of tretinoin on skin in terms of percentage. Finally, skin penetration of tretinoin was influenced by vehicle and concentration of this drug used in formulation

Use of Opuntia ficus-indica (L.) Mill extracts from Brazilian Caatinga as an alternative of natural moisturizer in cosmetic formulations

ABSTRACT The aim of this work was the obtainment of Opuntia fícus-indica (L.) Mill extract for the development of cosmetic formulations and in vivo evaluation of its moisturizing effects. The formulations were tested for preliminary and accelerated stability. Organoleptic characteristics, pH values and rheological behavior were assessed. The evaluation of moisturizing efficacy of the emulsions formulated with 3.0% of Polyacrylamide (and) C13-14 Isoparaffin (and) Laureth-7 containing 1.0 and 3.0% of O. ficus-indica hydroglycolic extract (EHG001) was performed using the capacitance method (Corneometer(r)) and the transepidermal water loss - TEWL evaluation (Tewameter(r)). The emulsions formulated were stable, exhibiting pseudoplastic and thixotropic behavior. The results of evaluation of moisturizing efficacy showed increased skin hydration after five hours by mainly increasing the skin barrier effect. The formulations containing 1.0 and 3.0% of EHG001 enhanced the skin barrier effect by reducing TEWL up to four hours after application. The results observed suggest that O. ficus-indica hydroglycolic extract may act through a humectant and occlusion mechanism

Development of mesalazine pellets coated with methacrylic-derived polymer

Mesalazine (5-ASA) is the standard drug for the treatment of inflammatory bowel disease (IBD) due to its local effect on intestinal and colonic mucosa. The effective and safe treatment of this disease requires more efficient delivery of the active substance to its site of action. The focus of this study was the use of multiparticulate systems, a modified release form in which the drug is divided into several functional subunits of release in the form of granules or pellets. When these forms are administered, they are rapidly disintegrated, distributing their content throughout the gastrointestinal tract. The aim of this study was to develop and evaluate a multiparticulate system consisting of pellets coated with polymer for pH-dependent release, derived from methacrylic acid and incorporated into the tablet dosage form of mesalazine as a model drug. The extrusion-spheronisation technique was used, resulting in smooth and spherical pellets with uniform size distribution, which were coated in fluidized bed using Opadry® Enteric 94K28327 containing Eudragit® S100 as the agent regulating drug release. The dissolution profile of coated pellets showed good control of drug release from the polymer at the two levels of coating evaluated (8% and 10%), but only the 10% coated pellets were statistically similar to Asalit® 400 mg.<br>A mesalazina (5-ASA) tem se apresentado como fármaco padrão para o tratamento da doença inflamatória intestinal (DII) devido ao seu efeito local na mucosa intestinal e colônica. A terapia efetiva e segura desta doença requer a chegada da substância ativa ao seu local de ação com maior eficiência. Nessa busca, tem se destacado o uso de Sistemas Multiparticulados, forma farmacêutica de liberação modificada, em que o fármaco está dividido em várias subunidades funcionais de liberação, sob a forma de grânulos ou péletes, que quando administrados, são rapidamente desintegrados distribuindo seu conteúdo por todo trato gastrintestinal. Este trabalho teve como objetivo desenvolver e avaliar péletes revestidos com polímero de liberação pH-dependente, derivado do ácido metacrílico, tendo como fármaco modelo a mesalazina. A técnica de extrusão-esferonização foi utilizada obtendo-se péletes lisos e esféricos com distribuição granulométrica uniforme, que foram revestidos em leito fluidizado utilizando Opadry® Enteric 94K28327 contendo Eudragit® S100 como agente regulador da liberação do fármaco. O perfil de dissolução dos péletes revestidos demonstrou bom controle na liberação do fármaco por parte do polímero nos dois níveis de revestimento avaliados (8 e 10%), porém, apenas os péletes revestidos a 10% demonstraram semelhança estatística com o medicamento de referência Asalit® 400 mg