Enhanced Ocular Anti-Inflammatory Activity of Ibuprofen Carried by an Eudragit RS100<sup>®</sup> Nanoparticle Suspension

Vol. 34, No. 5, 2002

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Original Paper

Enhanced Ocular Anti-Inflammatory Activity of Ibuprofen Carried by an Eudragit RS100^® Nanoparticle Suspension
Claudio Bucolo^a, Adriana Maltese^a, Giovanni Puglisi^b, Rosario Pignatello^b

^aBausch & Lomb - Fidia Oftal Pharmaceuticals, and
^bPharmaceutical Sciences Department, Catania University, Catania, Italy

Address of Corresponding Author

Ophthalmic Res 2002;34:319-323 (DOI: 10.1159/000065608)

Key Words

Ibuprofen
Nanoparticles
Drug delivery system
Eudragit RS 100
Rabbit eye

Abstract

Purpose: To investigate the ocular pharmacodynamic profile of a polymer nanoparticle system loaded with sodium ibuprofen (IBU-RS) in comparison to an aqueous solution 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 number of polymorphonuclear leukocytes in the aqueous humor were assessed after 2 h from arachidonate instillation. The ibuprofen concentration in the aqueous humor was evaluated by HPLC assay. The physico-chemical 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 number of polymorphonuclear leukocytes in the aqueous humor compared with the IBL formulation. Furthermore, the aqueous humor drug concentration 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 pharmacological 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 pharmacological activity.

Author Contacts

Dr. Claudio Bucolo
Bausch & Lomb-Fidia Oftal Pharmaceuticals
Corso Italia 141
I-95127, Catania (Italy)
Tel. +39 095 7221322, Fax +39 095 381580, E-Mail bucocla@unict.it

Article Information

Received: Received: May 6, 2002
Accepted after revision: July 8, 2002
Number of Print Pages : 5
Number of Figures : 3, Number of Tables : 0, Number of References : 13

Medline Abstract (ID 12381895)

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