Abstract

FORMULATION, CHARACTERIZATION AND EVALUATION OF SOLID DISPERSION FOR CNS DRUG LOADED IN TRANSDERMAL PATCH

Rajashree Gude*, Eliska D’Souza, Akshata Shirodker, Raunak Rai

Abstract

Bromocriptine Mesylate (BM) solid dispersion (SD) was formulated and loaded into matrix type transdermal patch, optimized and characterized. BM, an anti-Parkinson’s agent, belonging to BCS Class II, has low aqueous solubility and high permeability. Solubility and bioavailability was enhanced by SDs using Hydroxy propyl beta cyclodextrin (HP-b-C) and Hydroxy propyl cellulose (HPC), by Solvent evaporation and Kneading method. The SD was selected based on %yield, %drug content and in vitro dissolution data. The SD prepared by kneading method using combination of 2 carriers in a drug carrier ratio of 1: 0.5 :3 (F4), exhibited highest percentage yield of 97.640 ± 0.7692%, percentage drug content of 98.770 ± 0.8129 % and in vitro release 98.85 % in 60 mins. Hence, F4 was used. Concentration of HPMC K4M, Eudragit RL 100 and Propylene glycol were selected as independent variables for design of experiment (DoE) using 23 Full factorial design. A formula for 8 runs was generated, and formulated. Diffusion study and folding endurance were selected as dependent variables. Based on response data, a formula was generated for the optimized transdermal patch (E9) and evaluated for thickness, weight variation, %drug content, %elongation, folding endurance, surface pH, in-vitro diffusion study, ex-vivo permeation study and skin irritancy study. BM-SD transdermal patch was successfully developed with improved dissolution profile, avoidance of extensive firstpass metabolism, improved patient compliance, effective and safe for use.

Keywords: Bromocriptine Mesylate, Transdermal patch, Solid dispersion, Kneading method, 23 Full factorial design.