Formulation and evaluation of controlled release ocular inserts of betaxolol hydrochloride

Abstract

–Betaxolol Hydrochloride is a cardio selective β1 adrenergic receptor blocking agent used in the treatment of chronic open angle glaucoma and ocular hypertension In the present study, an attempt was made to formulate Betaxolol HCl ocular inserts. In matrix type the formulations for Betaxolol containing 10%, 12%, and 14% w/v of Gelatin, 1%, 1.5%, 2%, 2.5% and 3% w/v for Chitosan were prepared by solvent casting method and plasticizer were used in different concentration for smoothing texture of the ocular inserts. The prepared batches of ocular inserts were evaluated for weight variation thickness, drug content uniformity, swelling index. An increase in average weight and thickness is due to increase in polymer concentration. IR spectral studies were performed to confirm the interaction of drug with excipients. All formulations were tested for in vitro drug release (Simulated tear fluid) by vial method. The formulations GH8 and C5 show a maximum cumulative percentage drug release of 98.76% and 97.72% at the end of 12 th hrs, respectively. The drug release in all formulations decreases as the polymer concentration increases. The dissolution data of formulation were subjected to first order, Higuchi’s, and peppas equations. Drug release from the ocuserts by diffusion controlled mechanism. No significant change in the drug content and physical features was observed during storage at 25 0 C/60% RH and 40 0 C/75% RH for the selected formulation for three months. Keywords––Betaxolol Hydrochloride, Chitosan, Gelatin, Ocular inserts.