In Vitro and in Vivo Evaluation of Ezetimibe Fast-Dissolving Films

Abstract

Objective: The goal of this investigation was to develop and evaluate Ezetimibe fast-dissolving films, which are used to treat hyperlipidemia and prevent cholesterol absorption. Methods: The fast-dissolving Ezetimibe films were developed using the solvent casting method and included the following ingredients sodium carboxy methyl cellulose, HPMC E5, Polyvinyl Alcohol, Polyvinyl pyrrolidone which act as film-forming agents polyethylene glycol 600 and sodium starch glycolate, which acts as a superdisintegrant and plasticizer;, citric acid and stevia powder, which serves as a saliva stimulant and sweetener. Results: The fast-dissolving films of Ezetimibe prepared with PVP K30 released the drug up to 99.87% within 5 min, which showed the increased solubility, dissolution rate, flexibility and tensile strength of the films when compared to formulation prepared with sodium carboxy methyl cellulose, HPMC E5, Polyvinyl Alcohol. The FTIR and DSC studies were conducted for pure drug, polymers and optimized formulation E11, which indicated that were no incompatibilities found between the drug and polymers used in the present studies. Scanning electron microscopy analysis was performed for pure drug, and optimized formulation E11 showed that they were no surface fractures and cracks in the films. The optimized formulation E11 was subjected to in vivo studies by using New Zealand Rabbits, and accelerated stability studies revealed that all the formulation is stable. Conclusion: The current study reveals that fast-dissolving films formulated as a novel drug delivery technology can increase the solubility and dissolution rate of poorly water-soluble drug Ezetimibe.