Abstract

FORMULATION AND EVALUATION OF ERYTHROMYCIN LOADED NLCS TOPICAL GEL FOR THE TREATMENT OF ANTI-ACNE

C. K. Tyagi*, Bal Krishna Prajapati and Sunil Kumar Shah

ABSTRACT

NLCs (nanostructured lipid carriers) of erythromycin could be successfully prepared by the melt-emulsification and high-speed homogenization methods. In high-speed homogenization method produced smaller particles comparative with the melt-emulsification method. This study also indicates that the amount of liquid lipid and lecithin significantly affects the particle size as well as entrapment efficiency. It is also found that the release rate, permeation rate, and pharmacodynamics activity can be modulated upon changing the ratio of solid lipid to liquid lipid. The zeta potential value of drug-loaded NLC was found to be lower than the blank NLC, and this might be due to the sharing of charge of the drug on the lipid matrix. The release profile revealed that there is no significant effect on the method of preparation on the release of erythromycin from the NLC dispersions. The cumulative amount of the permeated drug at the end of 24 hrs was 3583.194, 3641.671, and 1495.940 µg/cm2 with a steady-state flux (Jss) of 171.56, 182.22, and 68.65 µg/cm2 /hr for NLC-F4G, NLC-F12G, and HF-G, respectively. The enhancement ratio was 2.50 and 2.65 for NLC-F4G and NLCF12G, respectively, as compared with the HF-G formulation. The results of the skin irritation study revealed that following seven days’ application of NLC-F4G, NLC-F12G, HF-G, and blank gel, there was no reaction found on the skin. Therefore, it can be assured that the gel formulation can be used for topical application. It can be concluded that the optimized NLC gels exhibit faster onset and prolonged action as compared to the marketed product.

Keywords: Acne, Erythromycin, melt-emulsification, transdermal permeability, Trans Dermal Delivery System.