Formulation of Tolmetin Ocuserts As Carriers for Ocular Drug Delivery System

Abstract

Background: Tolmetin (Tol) is a pyrrole acetic acid derivative that acts as a highly effective topical anti-inflammatory agent. Topical administration of Tol is effective for the management of ocular inflammations.The aim of this study was to formulate and improve a topical ophthalmic delivery system of Tol. Materials and methods: In the present study, ocular inserts of Tol were prepared using hydroxypropyl methylcellulose (HPMC) and carbomer 934p (CP). Ocular films were prepared with the objective of reducing the frequency of administration and obtaining controlled release to improve the anti-inflammatory drug delivery. Ocular films were subjected to investigations for their physical and mechanical properties, swelling behaviors, ex vivo bioadhesion, and in vitro drug permeability. Results: The physicochemical, bioadhesive, and swelling properties of films were found to vary significantly depending on the type and amount of polymers used and their combinations. The mixture of HPMC and CP films exhibited greater bioadhesion and showed higher ocular retentive time than the HPMC films. CP addition to the films significantly affected the properties of ocular inserts. HPMC to CP ratio (6:2.5) of ocular inserts sustained drug release for the longest span of 4 h. Conclusion: Tol can therefore be developed as an ocular insert delivery system for the treatment of ocular inflammation.