Development and Optimization of Levobunolol Hydrochloride In-situ Gel for Glaucoma Treatment

Abstract

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The aim of present study was to develop and optimize Levobunolol HCl in-situ gels for glaucoma treatment. Levobunolol HCl ophthalmic solution has been shown to be effective in intraocular pressure (IOP) and may be used in patients with chronic open-angle glaucoma or ocular hypertension. Levobunolol HCl in-situ gel was prepared using various concentrations of polymers such as Carbopol-940 (0.1, 0.2, 0.3 and 0.4% w/v), HPMC- E50LV (0.5, 1.0, 1.5 and 2.0 % w/v) and HPMC E4M (0.2, 0.4 and 0.6 %w/v) by pH induced gelling system with an objectives of increasing contact time, achieving controlled release, reduction in frequency of administration and greater therapeutic efficacy of drug. The prepared in-situ gels were then evaluated for their visual appearance, clarity, pH, drug content analysis, in-vitro gellation (Gelling strength), rheological studies, in-vitro drug release studies and sterility testing. It is evident from these studies that, formed polymeric in-situ gels had transparent, clear possessing satisfactory gelling strength. The drug contents of all optimized formulations were found to be from 99.38 - 99.71%. Formulations of our in-situ gels may possess the characteristics of pseudoplstic fluid. Method used for sterility testing was found to be reliable. Results of this study revealed that, formulations (F₂₁ and F₂₄) containing Carbapol-940 (0.2 and 0.3%) and HPMC E4M (0.4%) released their drug contents, 95.55 % and 90 % respectively, when compared to formulations (F₁₁ and F₁₅) containing Carbapol-940 (0.3 and 0.4%) and HPMC E50LV (1.5%) over a period of 480 minutes.