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Enhanced Ocular Anti-Inflammatory Activity of Ibuprofen Carried by an Eudragit RS100 Nanoparticle Suspension

Abstract

Purpose: To investigate the ocular pharmacodynamic profile of a polymer nanoparticle system loaded with sodium ibuprofen (IBU-RS) in comparison to an aq. soln. of ibuprofen lysinate (IBL) in the rabbit eye both being applied topically. Methods: Ocular inflammation was elicited by topical application of sodium arachidonate. Inflammation was quantified according to a modified Draize test. The protein level and the no. of polymorphonuclear leukocytes in the aq. humor were assessed after 2 h from arachidonate instillation. The ibuprofen concn. in the aq. humor was evaluated by HPLC assay. The physico-chem. properties of nanoparticles were also evaluated. Results: The IBU-RS nanosuspension formulation significantly reduced the primary signs of ocular inflammation as well as significantly reducing the protein level and the no. of polymorphonuclear leukocytes in the aq. humor compared with the IBL formulation. Furthermore, the aq. humor drug concn. from the group treated with IBU-RS was significantly higher compared to the IBL-treated group. The IBU-RS nanosuspensions showed very interesting size and surface charge values, adequate for ophthalmic administration. Conclusions: The pharmacol. profile of the topical IBU-RS nanosuspension formulation described in this study indicates that the dispersion of the drug within RS polymer nanoparticles increased its ocular bioavailability and ultimately its pharmacol. activity.

Autori

PUGLISI - Giovanni

PIGNATELLO - Rosario

Altri Autori

Bucalo Claudio
Maltese Adriana