Abstract

OPTIMIZATION AND IN VIVO EVALUATION OF TIMOLOL MALEATE IN SITU GELS FOR OCULAR DRUG DELIVERY

Shiva Kumar Yellanki*, Balaji Anna and Marupaka Radha Kishan

ABSTRACT

The objective of the study was to develop optimized formulation of In situ gel of Timolol maleate (TM) antiglaucoma agent using pH and Ion activated polymers Carbopol 940 and Sodium alginate respectively as gelling agents, Hydroxy Propyl Methyl Cellulose (HPMC K4M) as viscosity enhancing polymer. The 23 factorial design was employed to optimize the formulation considering Carbopol 940, Sodium alginate and Hydroxy Propyl methyl cellulose (HPMC K4M) as independent variables, Sol to gel transition time (sec) and In vitro percentage drug release as dependent variables. Formulations were prepared successfully and assessed for appearance, gelling capacity, pH, drug content and in vivo ocular irritation. Based on sol to gel transition time (sec) and in vitro percentage drug release F9 formulation was found to be best optimized formulation from the nine formulations developed by 23 factorial design. The study revealed that the in situ gel system of TM sustained the antiglaucoma activity up to 8 h for F9 formulation.

Keywords: Timolol maleate, Two-level factorial design, In situ gel system, Antiglaucoma activity.