Transbuccal Delivery of Spray Dried Lovastatin From Mucoadhesive Buccal Patches and in Vitro Characterization

Abstract

Objective: The aim of the present work was to develop and characterize mucoadhesive film of spray dried Lovastatin (LVS) for buccal delivery to enhance bioavailability.
 Methods: Mucoadhesive films were prepared by solvent casting technique by using different polymers HPMCK4M, HPMC E5LV and chitosan. The successful patches were evaluated for film thickness, weight, content uniformity, surface pH, swelling index, folding endurance, ex-vivo residence time, ex-vivo bioadhesion test, in vitro drug release, ex-vivo drug permeation and stability study.
 Results: The thickness of all prepared patches ranged from 0.21±0.07 to 1.5±0.39 mm, the weight of the film 89.10±0.6 to 128.57±0.3 mg, drug content 85.47±0.87 to 97.33±0.31%, surface pH 5.6±0.67 to 7.6±0.98, swelling index 23.0±4.1 to 76.5±3.6%, folding endurance 165±1.9 to 350±2.5 respectively. Ex-vivo residence time ranged from 2.2±0.08to 8.2±0.17 h and ex-vivo bioadhesive strength 30±0.64 to 66±0.43 g. The formulations with HPMC E5 shown short period of residence time and shows weak force of adhesion., which might be because of low viscosity of the polymer which resulted into weak adhesion. The percentage drug release and ex-vivo drug permeation was in the following descending order HPMC K4M>HPMC E5LV>chitosan. These results confirm the extension of drug release in case of ionic polymer chitosan. The kinetics data shows that drug release and permeation follows nonfiction diffusion. Accelerated stability data revealed that there is no significant change in drug content, in vitro drug release and ex-vivo permeation.
 Conclusion: It can be concluded that mucoadhesive buccal patch is a promising dosage form to enhance the drug bioavailability by preventing first-pass metabolism thus providing better therapeutic efficacy.