Acta Pharm. 55 (2005) 305-314[ Full paper in PDF ]
Pefloxacin mesylate is a flouroquinolone antibacterial drug effective in the treatment of bacterial conjunctivitis. The objective of the present work was to develop ocular inserts of pefloxacin mesylate and evaluate their potential for sustained ocular delivery. Reservoir-type ocular inserts were prepared by the film casting technique in teflon coated Petri dishes and characterized in vitro by drug release studies using a flow-through apparatus that simulated the eye conditions. Six formulations were developed, which differed in the ratio of polymers Eudragit RS 100 and Eudragit RL 100 used for the preparation of the rate controlling membrane. All formulations carried 0.72 mg pefloxacin mesylate, 2.69 mg polyvinyl pyrrolidone (PVP) K-30, plasticizers, propylene glycol (10% m/m) and dibutyl phthalate (15%, m/m). The optimized formulation was subjected to microbiological studies, in vivo studies, interaction studies, and stability studies to assess the effectiveness of the formulation. Cumulative drug released from the formulation ranged from 90-98% within 48 to 120 hours.
On the basis of in vitro drug release studies, the formulation with Eudragit RS 100/Eudragit RL 100 (4:1) was found to be better than the other formulations and it was selected as an optimized formulation. On the basis of in vitro, microbiological, in vivo drug release, interaction and stability studies, it can be concluded that this ocular insert formulation provided the desired drug release in vitro for 5 days and remained stable and intact at ambient conditions.
Keywords: pefloxacin mesylate, ocular insert, in vitro release studies, in vivo studies