Enhanced ocular anti-inflammatory activity of ibuprofen carried by an Eudragit RS100 nanoparticle suspension.
OBJECTIVE
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.
Bucolo
Claudio
C
Bausch & Lomb--Fidia Oftal Pharmaceuticals, Catania, Italy. bucocla@unict.it
Maltese
Adriana
A
Puglisi
Giovanni
G
Pignatello
Rosario
R
D000180:Acrylic Resins / Q000627:therapeutic use*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000627:therapeutic use*; D001082:Aqueous Humor / Q000166:cytology / Q000378:metabolism; D003231:Conjunctivitis / Q000188:drug therapy / Q000473:pathology; D009877:Endophthalmitis / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D005136:Eye Proteins / Q000378:metabolism; D006940:Hyperemia / Q000188:drug therapy / Q000473:pathology; D007052:Ibuprofen / Q000627:therapeutic use*; D007499:Iris Diseases / Q000188:drug therapy / Q000473:pathology; D007500:Iritis / Q000188:drug therapy / Q000473:pathology; D008297:Male; D036103:Nanotechnology; D009504:Neutrophils / Q000473:pathology; D010316:Particle Size; D011817:Rabbits; D013535:Suspensions
D000180:Acrylic Resins; D000894:Anti-Inflammatory Agents, Non-Steroidal; D005136:Eye Proteins; D013535:Suspensions; C050528:Eudragit RS; D007052:Ibuprofen