Preparation and evaluation of sustained ophthalmic gel of enoxacin

Drug Dev Ind Pharm. 2005 Dec;31(10):969-75. doi: 10.1080/03639040500306203.

Abstract

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.

MeSH terms

  • 2-Hydroxypropyl-beta-cyclodextrin
  • Algorithms
  • Animals
  • Anti-Infective Agents / administration & dosage*
  • Anti-Infective Agents / pharmacokinetics
  • Anti-Infective Agents / toxicity
  • Aqueous Humor
  • Area Under Curve
  • Chemistry, Pharmaceutical
  • Cornea / chemistry
  • Cornea / metabolism
  • Delayed-Action Preparations
  • Drug Compounding
  • Enoxacin / administration & dosage*
  • Enoxacin / pharmacokinetics
  • Enoxacin / toxicity
  • Excipients
  • Eye / metabolism
  • Hypromellose Derivatives
  • In Vitro Techniques
  • Irritants
  • Linear Models
  • Methylcellulose / analogs & derivatives
  • Methylcellulose / chemistry
  • Microdialysis
  • Pharmaceutical Vehicles
  • Rabbits
  • beta-Cyclodextrins / chemistry

Substances

  • Anti-Infective Agents
  • Delayed-Action Preparations
  • Excipients
  • Irritants
  • Pharmaceutical Vehicles
  • beta-Cyclodextrins
  • 2-Hydroxypropyl-beta-cyclodextrin
  • Enoxacin
  • Hypromellose Derivatives
  • Methylcellulose