Fabrication, Physicochemical and Pharmaceutical Characterization of Losartan Potassium–Loaded Buccal Films

Introduction:Buccal films for anti-hypertensive drugs like losartan potassium can avoid hepatic first-pass metabolism, improve bioavailability, and enhance patient compliance.Objective: The purpose of this study was to develop and characterize buccal films of losartan potassium, to achieve sustained and complete release and permeation of the drug over a reasonable period, without the risk of the film being dislodged from buccal mucosa during use.Method: Buccal films with different ratios of hydrophilic (HPMC K15M), hydrophobic polymers (Eudragit RL 100) (1:1, 2:1, and 3:1), along with a fixed percentage of drug loading and mucoadhesive polymer Carbopol 934P, were developed using the solvent casting technique.The films were subjected to in -vitro analyses and tests to assess their physicochemical, mechanical, and pharmaceutical properties.Results: The films were found to be satisfactory regarding handling characteristics, mechanical properties, swelling index, mucoadhesivity, in -vitro release, and permeation.In vitro drug release and permeation studies (across dialysis membrane) in simulated saliva (pH 6.8) using a Franz diffusion cell revealed that films containing HPMC K15M and Eudragit RL100 in a ratio of 3:1 could sustain the release of losartan potassium for 6 hrs, achieving a release of 95.390.37%,as well as a permeation of 98.382.08%drug occurred across synthetic membrane in 6 hrs.Interpretation of kinetic modeling of release, permeation, and diffusional transport mechanism data indicates Higuchi kinetics, matrix formation with non-Fickian transport, and a constant rate of permeation.The permeability coefficient, steady-state flux values, and kinetics of release and permeation showed that the film is the most suitable for further development and clinical application.Conclusion: HPMC K 15M and Eudragit RL 100 in a ratio of 3 :1 could form a swellable matrix from which maximum release of losartan potassium occurred within 6 hrs, and with a constant rate of permeation across the synthetic membrane, attaining completion in 6 hrs.Thus, this composition is likely to produce similar results in vivo and has a promising prospect for commercialization.