Preparation and evaluation of sustained ophthalmic gel of enoxacin.
The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid precorneal elimination of the drug may be overcome by the use of a gel system. The present work describes the formulation and evaluation of an ophthalmic delivery system containing an antibacterial agent, enoxacin, based on the concept of ophthalmic sustained gel, in which 2-hydroxypropyl-beta-cyclo-dextrin (HP-beta-CD) was used as a penetration enhancer in combination with hydroxypropylmethylcellulose (Methocel F4M) which acted as a vehicle. The developed formulation was therapeutically efficacious, nonirritant, and provided sustained release of the drug over 8 h period in vitro and 7 h period in vivo. The developed system is a viable alternative to conventional eye drops.
Liu
Zhidong
Z
Department of Pharmaceutical, Shenyang Pharmaceutical University, Shenyang, P.R. China.
Pan
Weisan
W
Nie
Shufang
S
Zhang
Libo
L
Yang
Xinggang
X
Li
Jiawei
J
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000465:Algorithms; D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000633:toxicity; D001082:Aqueous Humor; D019540:Area Under Curve; D002626:Chemistry, Pharmaceutical; D003315:Cornea / Q000737:chemistry / Q000378:metabolism; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D015365:Enoxacin / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000633:toxicity; D005079:Excipients; D005123:Eye / Q000378:metabolism; D065347:Hypromellose Derivatives; D066298:In Vitro Techniques; D007509:Irritants; D016014:Linear Models; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D017551:Microdialysis; D014677:Pharmaceutical Vehicles; D011817:Rabbits; D047392:beta-Cyclodextrins / Q000737:chemistry
D000890:Anti-Infective Agents; D003692:Delayed-Action Preparations; D005079:Excipients; D007509:Irritants; D014677:Pharmaceutical Vehicles; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D015365:Enoxacin; D065347:Hypromellose Derivatives; D008747:Methylcellulose