In vitro penetration activity of ionic liquid-Gnetum gnemon seed extract loaded solid lipid nanoparticles

Gnetum gnemon L. (Melinjo) seeds have high trans-resveratrol, which was known to have poor skin absorption ability.This study was performed to evaluate the skin absorption of ionic liquid-melinjo seed extract (IL-MSE) loaded solidlipid nanoparticles (SLN). The SLNs was formulated with glyceryl monostearate as the lipid ingredient, ceteareth-25,ceteareth-6, stearyl alcohol, an aqueous phase, and 10% melinjo seed extract. The SLNs were prepared by modificationof high-pressure homogenization. The polydispersity index (PDI), zeta potential, entrapment efficiency (EE), particlesize (PS), and morphological scanning electron microscopy (SEM) were evaluated. The in vitro penetration of IL-MSESLN was carried out by using the Franz cell diffusion method. The SLNs formulations showed an average of particlessize about 794 nm, and with high lipid and surfactant, the content could contributing to high entrapment efficiencyto almost 89%. Even though the polydispersity index of SLN was 1.229, and zeta potential measurement was 62.56mV. Up to 45% of the trans-resveratrol penetrated through the skin after 8 hours of the test run. The IL-MSE loadedto SLNs could improve the absorption of trans-resveratrol through the skin.

Performance evaluation of Cryo Laser Phoresis technique as biophysical method to promote diclofenac sodium cutaneous perfusion

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.