Formulation and In Vitro Evaluation of Novel Sustained Release and Bioadhesive Gastroretentive Drug Delivery System For An Anti-Viral Drug

Abstract

Aciclovir is a potent anti-herpal agent with shorter half-life and poor oral bioavailability due to erratic and pH dependant absorption, more at acidic pH. Therefore, the purpose of this research is to formulate and optimize the gastro retentive mucoadhesive formulation of Aciclovir IP, so that the drug is retained at the absorption site for increased duration which in turn helps for better absorption and releases drug in a sustained manner. A natural mucoadhesive gum (Extract A) extracted from fruits of Aegle marmelos is used along with synthetic mucoadhesive polymers like HPMC K15M, Carbopol 971P in different proportions. The physicochemical compatibility of the drug and the polymers was studied by FTIR spectroscopy. The results suggested no physicochemical incompatibility between the drug and the polymers. On the prepared formulations various physicochemical tests, in vitro drug release and ex vivo mucoadhesion studies were carried out. Results indicate formulation (F7) that contains HPMC K15M and Natural polymer found to be releasing drug in a sustained manner (96.46±0.76%) for 12 h with good mucoadhesive property. From the results F-7 was taken as best formulation and is subjected to stability studies (30±2 °C / 65±5% RH) for 60 days. The stability studies showed that there was no significant change found in physicochemical properties, in vitro release and ex vivo mucoadhesion studies.