Original Articles
Revathy V. Nair, Sreeja C. Nai
Abstract
Conventional ocular preparation like eye drop, solutions or suspensions often result in poor bioavailability and patient compliance. Timolol maleate is a beta adrenoceptor blocker widely used in treatment of glaucoma in the form of eye drop. The study aimed in preparing Timolol Maleate ocular inserts (ocuserts) enhancing ocular bioavailability and the reduction in the frequency of instillation thereby resulting in better patient compliance. Timolol maleate ocuserts were prepared by using solvent casting method using a hydrophilic polymer (Sodium alginate) and polyethylene glycol as a plasticizer. Six different ocuserts (F1-F6) were evaluated for pH, weight variation, thickness, folding endurance, percentage drug content, moisture absorption, moisture loss, in-vitro drug release by using dialysis membrane. In-vitro drug release data of optimized formulation (F4) was treated according to Zero, First, Korsmeyer Peppas and Higuchi kinetics to access the mechanism of drug release. Its sterility test was performed based on IP guidelines. From the parameters, the ideal formulation was identified as F4 with pH (7.4), weight variation(5.50 mg), thickness(0.085 mm), folding endurance (89), percentage drug content (97.27%), moisture absorption(4.17%), moisture loss(3.42%), in-vitro drug release (95% at 10 hours). F4 showed first order release pattern. The sterility test of ocusert F4 was performed by using alternate thioglycollate medium and soyabean casein digest medium, which confirmed that the ocusert F4 passed the sterility test and hence they are sterile preparations. Thus the developed optimized ocusert with its sustained release property can be utilized as an alternative to conventional dosage form for the treatment of Glaucoma