Flurbiprofen loaded biodegradable nanoparticles for ophtalmic administration.
Poly(lactic/glycolic) acid nanoparticles incorporating flurbiprofen (FB) were prepared by the solvent displacement technique using poloxamer 188 as a stabilizer to improve the availability of the drug for the prevention of the inflammation caused by ocular surgery. A 2(3) + star design was applied to investigate the influence of several factors such as the pH of the aqueous phase, the initial concentration of the stabilizer, and the drug used to prepare the nanoparticles (NPs) on the physicochemical properties (particle size analysis, zeta potential, and drug loading efficiency) of the colloidal system. The best formulations were those prepared at pH 3.5 with a concentration of 1.5 mg/mL of FB and 10 or 20 mg/mL of poloxamer 188. These formulations showed an appropriate average size for ophthalmic administration (232.8 and 277.6 nm, respectively) and a good yield of entrapment efficiency (94.60% and 93.55%, respectively). The release behavior of FB from the developed NPs was complete and exhibited a biphasic pattern. Formulations did not show toxicity on ocular tissues. In vivo anti-inflammatory efficacy was assessed in the rabbit eye after topical instillation of sodium arachidonate (SA). A higher decrease of the SA-induced inflammation was obtained for the NP formulations.
Vega
E
E
Department of Physical Chemistry, Faculty of Pharmacy, Avda. Joan XXIII s/n, 08028 Barcelona, Spain.
Egea
M A
MA
Valls
O
O
Espina
M
M
García
M L
ML
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000009:adverse effects; D001711:Biotransformation; D002021:Buffers; D004339:Drug Compounding; D004563:Electrochemistry; D005123:Eye / Q000187:drug effects; D005480:Flurbiprofen / Q000008:administration & dosage* / Q000009:adverse effects; D007509:Irritants; D019344:Lactic Acid; D053758:Nanoparticles; D009883:Ophthalmic Solutions; D010316:Particle Size; D010710:Phosphates; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers; D011817:Rabbits; D012996:Solutions; D013501:Surface-Active Agents
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002021:Buffers; D007509:Irritants; D009883:Ophthalmic Solutions; D010710:Phosphates; D011108:Polymers; D012996:Solutions; D013501:Surface-Active Agents; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D005480:Flurbiprofen