Development, In-Vitro and Ex-Vivo Evaluation of Muco-adhesive Buccal patches of Candesartan cilexetil

Abstract

Candesartan cilexetil (CC), is an anti-hypertensive drug belongs to angiotensin-II receptor antagonist. CC possesses poor oral bioavailability due to first-pass metabolism and poor aqueous solubility. Various approaches are known to reduce the problems of first-pass metabolism. Hence, buccal drug delivery was an approach to improve bioavailability. The present study, buccal muco-adhesive patches were prepared by using hydroxyl propyl methyl cellulose (HPMC E15) and eudragit RLPO and evaluate for physicochemical properties, such as thickness, weight uniformity, folding endurance, drug content, surface pH, swelling index, moisture absorption and ex vivo permeation studies. Among all the formulations, F7 was selected as an optimized formulation and was found to be 100.55% of drug in 6 hrs, and exhibited controlled drug release, follows zero-order kinetics with diffusion as a release mechanism. The ex-vivo permeation studies revealed that 100% of drug permeated in 6 hrs. Therefore, the buccal patches of CC were successfully developed and enhancement in oral bioavailability is further confirmed by conducting in-vivo studies.