FORMULATION DEVELOPMENT AND CHARACTERIZATION OF TRANSDERMAL FILMS OF LERCANIDIPINE FROM ACRYLIC FILMS

The purpose of this research was to develop a matrix diffusion type transdermal therapeutic system containing drug Lercanidipine with a blend of eudragit RL 100 and eudragit RS 100 as polymer system by the solvent evaporation technique with PEG 400 as plasticizer. Glycerin was used as enhance the transdermal permeation of Lercanidipine. Eight formulations with varied concentration of polymers, plasticizers and permeation enhancers were done and optimization of the concentration of formulation components was performed. Formulated transdermal films were evaluated for various physicochemical parameters, in vitro release, and stability studies. Good uniformity of the drug content among the patches was observed for all the formulations which ranged from 94.75% to 98.42%. Formulation variables such as polymer ratio, concentration of plasticizer and permeation enhancers were found to influence the in vitro drug release behavior of the formulated patches. Increasing the concentration of eudragit RL 100 and plasticizer, the presence of permeation enhancers were found to increase the in vitro drug release of the formulated patches. The total amount of drug released from the films over 8 and 24 hours followed the order: 10% w/w Glycerin > 10% w/w PEG 400 > 5% w/w Glycerin > 5 % w/w PEG 400. Based on the physicochemical and drug release characteristics, the eudragit films with polyethylene glycol 400 and glycerin are suitable to design matrix diffusion type transdermal system for Lercanidipine and the F8 formulation with eudragit RL 100 to eudragit RS100 ratio 1:1, 5% w/w glycerin as permeation enhancer and 5% w/w PEG 400 as plasticizer showed a thickness of 0.260mm and drug loading of 3.912mg/ cm2 was considered as the best formulation. The cumulative percentage amount of drug release from the F8 formulation film was found to be 38.381% at the end of 8 hours and 58.154% at the end of 24 hours. The films were found to be stable during the entire stability period of 60 days at 45ºc