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Development of an In Vitro Ocular Platform to Test Contact Lenses
Published on: April 6, 2016
Ocular inserts for controlled delivery of pefloxacin mesylate: preparation and evaluation
Yasmin Sultana1, Mohammad Aqil, Asgar Ali
1Department of Pharmaceutics Faculty of Pharmacy, Hamdard University New Delhi-110062, India. yas2312003@yahoo.com
Abstract:
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.
Insights
This study developed sustained-release ocular inserts for pefloxacin mesylate, an antibiotic for bacterial conjunctivitis. The optimized formulation demonstrated stable, intact drug delivery for five days in simulated eye conditions.
Area of Science:
- Ophthalmology
- Pharmaceutics
- Drug Delivery
Background:
- Bacterial conjunctivitis requires effective and sustained ocular drug delivery.
- Pefloxacin mesylate is a potent fluoroquinolone antibacterial agent.
- Current treatments may lack sustained release, necessitating improved formulations.
Purpose of the Study:
- To develop and evaluate ocular inserts for sustained delivery of pefloxacin mesylate.
- To optimize the polymer ratio for controlled drug release.
- To assess the in vitro, microbiological, in vivo, and stability profiles of the developed inserts.
Main Methods:
- Reservoir-type ocular inserts were fabricated using the film casting technique.
- Formulations varied in the ratio of Eudragit RS 100 and Eudragit RL 100 polymers.
- In vitro drug release studies were conducted using a flow-through apparatus simulating ocular conditions.
Main Results:
- Six formulations were prepared, all containing pefloxacin mesylate, polyvinyl pyrrolidone (PVP) K-30, and plasticizers.
- The formulation with an Eudragit RS 100/Eudragit RL 100 ratio of 4:1 exhibited optimal sustained release.
- Cumulative drug release reached 90-98% over 48 to 120 hours, with the optimized insert remaining stable for 5 days.
Conclusions:
- The developed ocular insert formulation provides sustained in vitro release of pefloxacin mesylate for up to 5 days.
- The optimized formulation demonstrated stability and effectiveness under ambient conditions.
- These ocular inserts show significant potential for managing bacterial conjunctivitis through prolonged drug delivery.
