Development, Optimization and Evaluation of Buccal Film for Management of Hypertension Using BCS Class I Drug

Abstract

The primary aim of the work was to design an immediate release mucoadhesive buccal film for the management of hypertension. Sildenafil citrate is provided very prominent result in pulmonary hypertension. The bioavailability of sildenafil citrate is approximately 43 % when administered orally in the form of tablet with a dose of 20 mg. which is much lesser than the other hypertensive agents. So, keeping in mind the pharmacokinetics profile of the sildenafil citrate, an alternate site of administration had to be designed. The main focus of the formulation is to increase the bioavailability of the molecule. The Preformulation study was carried out to check the purity and compatibility of the sildenafil with both the polymers (Proloc and Methocel E5 LV). The FT-IR and DSC graph proved that drug and polymers are good compatible with each other. The preliminary trials batches were formulated by changing the concentration of polymers and plasticizers with a different ratio. Observed the all 85 primary batches and select the working range of the polymers and plasticizers. The optimisation was done with the help of the design expert software by applying 32 full-factorial design. All the batches are evaluated for the various parameters to obtain the final optimised batch. The final optimised formula was selected based on the overlay plot. The drug-loaded film was prepared and evaluated for the physical and mechanical parameters like; thickness, disintegration time, tensile strength, elongation, swelling index, content uniformity, dissolution test, in-vitro drug release profile and in-vitro permeation profile. The research proved that the immediate release buccal film of sildenafil citrate possesses good bioavailability as compared to the marketed oral tablet formulation and has good market potential.