Design and evaluation of ocular drug delivery system for controlled delivery of gatifloxacin sesquehydrate: In vitro and in vivo evaluation.
The objective of this investigation was to formulate ocular inserts of gatifloxacin sesquehydrate to achieve controlled drug release. Drug reservoir was prepared using hydrophilic polymers, namely polyvinyl alcohol and polyvinyl pyrrolidone. The rate controlling membrane was prepared using hydrophobic ethyl cellulose by solvent casting method. Ocular inserts were evaluated for uniformity of weight, thickness, drug content, surface pH, percentage moisture absorption, percentage moisture loss, drug excipients compatibility, in vitro release, sterility test, eye irritation, in vivo release, microbiological and stability studies. Ocular inserts complied with all the physico-chemical parameters. Drug excipients compatibility studies demonstrated no interaction between drug and polymer. The in vitro release profile of drug from ocular inserts showed controlled and prolonged release. The release data followed zero order and non-Fickian transport. Ocular inserts passed the test for sterility. Correlation between in vitro and in vivo drug release was found to be strong revealing the efficacy of the formulation. The drug was found to be effective against Staphylococcus aureus and Escherichia coli. The result of accelerated stability study revealed no significant change in drug content of promising formulation.
Patel
Upendrakumar L
UL
Arihant School of Pharmacy & Bioresearch Institute, Gandhinagar, Gujarat, India.
Chotai
Narendra P
NP
Nagda
Chirag D
CD
D000269:Adhesives; D000465:Algorithms; D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D002152:Calorimetry, Differential Scanning; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D003993:Dibutyl Phthalate / Q000737:chemistry; D004058:Diffusion; D016503:Drug Delivery Systems; D015195:Drug Design; D004355:Drug Stability; D005123:Eye; D024841:Fluoroquinolones / Q000008:administration & dosage* / Q000009:adverse effects / Q000494:pharmacology; D000077734:Gatifloxacin; D005990:Glycerol / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D007509:Irritants; D008567:Membranes, Artificial; D008826:Microbial Sensitivity Tests; D009883:Ophthalmic Solutions; D010968:Plasticizers; D011092:Polyethylene Glycols; D011142:Polyvinyl Alcohol; D011145:Polyvinyls; D011759:Pyrrolidines; D011817:Rabbits; D017550:Spectroscopy, Fourier Transform Infrared; D013242:Sterilization
D000269:Adhesives; D000890:Anti-Infective Agents; D003692:Delayed-Action Preparations; D024841:Fluoroquinolones; D007509:Irritants; D008567:Membranes, Artificial; D009883:Ophthalmic Solutions; D010968:Plasticizers; D011145:Polyvinyls; D011759:Pyrrolidines; C505150:poly(N-vinylpyrrolidine); D003993:Dibutyl Phthalate; D011092:Polyethylene Glycols; C013517:ethyl cellulose; D011142:Polyvinyl Alcohol; D002482:Cellulose; D000077734:Gatifloxacin; D005990:Glycerol