Quality by Design Approach in Formulation Development and Evaluation of in Situ Ophthalmic Gel of Olopatadine HCL

Abstract

Objective: The aim of present study was to apply Quality by Design (QbD) for development of an optimized ion sensitive in situ ophthalmic gel Olopatadine HCl to increase drug residence time, ocular bioavailability and decreased dosing frequency of drug administration. Method: To develop the optimized formulation, 3 2 full factorial design method was adopted. The material attributes and critical quality attributes of the in situ gel were identified. Materials attributes were amount of Sodium Alginate and HPC and CQA's identified were % drug release and viscosity. The formulations were assessed for appearance, gelling ability, sterility, pH, drug content, viscosity, drug release through cellophane membrane, drug release through corneal membrane of goat, and stability study as per ICH guidelines. Formulations F3 and F8 were selected and were again analysed by grid analysis. Result: The optimized batches exhibited all results in acceptable limits. F8 was found to be the best formulation from the nine formulations developed by 3 2 full factorial design. The optimized formulation showed better drug release when compared with marketed formulation. Conclusion: The study revealed that the in situ gelling system of Olopatadine HCl sustained the effect of drug up to 10 hours. The formulation F8 extended the release of drug up to 10 hours as compared to marketed preparation of Olopatadine HCl, Zyopta (solution), which gives 98.39% drug release within 6 hours.

Potential of Stimuli-Responsive In Situ Gel System for Sustained Ocular Drug Delivery: Recent Progress and Contemporary Research

“…In another similar study, Carbopol 974 was utilized as a gelling agent in formulating olopatadine hydrochloride to treat allergic conjunctivitis. Two optimized formulations were selected in this study with (F3) 0.1% w / v Carbopol 974 and 1.0% w / v HPMC E50LV and (F7) 0.3% w / v Carbopol 974 and 0.6% w / v HPMC E50LV with appropriate gelling capacity within a pH increasing environment after 3–4 h [ 73 ]. Both optimized formulations have a free flow characteristic in slightly acidic pH.…”

Formulation and Evaluation of Besifloxacin Loaded In Situ Gel For Ophthalmic Delivery

“…In eye drug is administered at various site such as cornea, conjunctiva and sclera for better achievement of bioavailability and required effects related with the therapy. The drugs for allergies, glaucoma, bacterial infections, conjunctivitis, keratitis, local anaesthetics and viral infection can be administered at suitable sites in the eye 1 .…”

Sistem Penghantaran Sediaan Optalmik dengan Insitu Gel

“…Formula yang optimum terdiri dari carbopol 974 dengan konsentrasi 0,3% b/v dan HPMC E50LV dengan konsentrasi 1% w/v menghasilkan gel yang jernih, memiliki kapasitas gel yang baik, steril dan pelepasan obat lebih dari 6 jam. Formula tersebut menghasilkan gel yang jernih pada uji kejernihan dengan pH 7,437 .…”