Nanoemulsions as vehicles for transdermal delivery of glycyrrhizin

Abstract

The present investigation aims to evaluate an isotropic and thermodynamically stable nanoemulsion formulation for transdermal delivery of glycyrrhizin (GZ), with minimum surfactant and cosurfactant (Smix) concentrations that could improve its solubility, permeation enhancement, and stability. Pseudoternary phase diagrams were developed and various nanoemulsion formulations were prepared using soyabean oil as oil, Span 80, Brij 35 as a surfactant and isopropyl alcohol as a cosurfactant. Nanoemulsion formulations that passed the thermodynamic stability tests were characterized for pH, viscosity and droplet size using a transmission electron microscopy. The transdermal ability of glycyrrhizin through human cadaver skin was determined using Franz diffusion cells. The in vitro skin permeation profile of the optimized nanoemulsion formulation (NE2) was compared to that of conventional gel. A significant increase in permeability parameters such as steady-state flux (Jss) and permeability coefficient (Kp) was observed in the optimized nanoemulsion formulation (NE2), which consisted of 1% wt/wt of mono ammonium glycyrrhizinate (MAG), 32.4% Span 80, 3.7% Brij 35, 10% isopropyl alcohol, 46.5% soyabean oil and 6.4% distilled water. No obvious skin irritation was observed for the studied nanoemulsion formulation (NE2) or the gel. The results indicated that nanoemulsions are promising vehicles for transdermal delivery of glycyrrhizin through human cadaver skin, without the use of additional permeation enhancers, because excipients of nanoemulsions act as permeation enhancers themselves.Uniterms: Nanoemulsions/use/in vitro skin permeation. Glycyrrhizin/transdermal delivery. Isotropic nanoemulsion formulation/evaluation. Anti-inflammatories/transdermal delivery. Surfactants. Permeation/ enhancers/in vitro study.O objetivo da investigação é avaliar uma nanoemulsão isotrópica termodinamicamente estável para a administração transdérmica da glicirrizina (GZ), com concentrações mínimas de tensoativo e co-tensoativo (Smix), que poderiam melhorar a sua solubilidade, a permeação e a estabilidade. Os diagramas pseudoternários de fase foram desenvolvidos e diversas nanoemulsões foram preparadas com óleo de soja como óleo, Span 80, Brij 35 como tensoativos e álcool isopropílico como co-tensoativo. As nanoemulsões que passaram por testes de estabilidade termodinâmica foram caracterizadas por pH, viscosidade, tamanho de gota e microscopia eletrônica de transmissão. A capacidade transdérmica da glicirrizina em passar através da pele de cadáver humano foi determinada por células de difusão de Franz. O perfil in vitro de permeação cutânea da formulação otimizada (NE2) foi comparada com a de gel convencional. Observouse aumento significativo nos parâmetros de permeabilidade, como fluxo de equilíbrio (JSS) e coeficiente de permeabilidade (Kp) na formulação otimizado (NE2), que consistiu de 1% wt/wt de monoglicirrizinato de amônio (MAG), 32,4% de Span 80, 3,7% de Brij 35, 10% de álcool isopropílico, 46,5% de óleo de soja e 6,4% de água destilada....

Antimicrobial Activity of Curcumin-Loaded Myristic Acid Microemulsions against <i>Staphylococcus epidermidis</i>

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Effects of Carbopol^&reg; 934 proportion on nanoemulsion gel for topical and transdermal drug delivery: a skin permeation study

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“…33,34 Moreover, differences in fluorescence signals among the NGs showed that the proportion of CP934 influenced the skin permeation rates by altering the main skin permeation routes. There are three major routes for drug penetration into the subepidermal tissue: hair follicles together with their sebaceous glands, sweat ducts, and the SC (including transcellular and intercellular routes).…”

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“…As shown in Fig. 3 the maximum emulsification region was obtained in Smix (4:1) with Soyabean oil, Smix (5:1) with acid ester and Smix (4:1) with Soyabean oil base ester concentration in respectively 37 . …”