Design and evaluation of esmolol hydrochloride ocular inserts with special reference to glaucoma treatment

摘要

In developing a drug delivery strategy, issues of absorption, distribution, metabolism, and elimination must be considered. The eye presents unique opportunities and challenges when it comes to the delivery of pharma-ceuticals. While absorption by this route is bungling, there are few side effects with conventional ocular dosage forms. Hence, ocular inserts were prepared with prolonged release of drug and minimum swelling within cul-de-sac using esmolol HC1 drug the work focuses on treatment of glaucoma by formulating ocular inserts. By using different polymeric combination of esmolol HC1 using hydroxy-propyl methyl cellulose (HPMC 3-5 %), chitosan (3-5 %), polyvinyl alcohol (PVA 3-5 %), methyl cellulose (3-5 %) as polymer by solvent casting technique with objective of increasing contact time, achieving controlled release, reduction on frequency of administration and greater therapeutic efficiency. The prepared ocular insert were then evaluated for physical appearances tensile strength, % elongation at break, stress, weight variation, uniformity of thickness, % moisture absorption, surface pH, folding endurance, Fourier transform infrared spectroscopy, in-vitro transcorneal permeation studies etc. It is evident from these study that formed polymeric ocular insert have appreciable strength and safety. Physicochemical characterization and in vitro transcorneal permeation studies revels that, the prepared ocular insert formulation F2 and F8 containing HPMC and PVA had release their drug content, 98.54 and 97.24 respectively over a extended period of 24 h. Hence these formulation selected as best optimized formulation.