Design and evaluation of polymeric ocular drug delivery system for controlled delivery of moxifloxacin hydrochloride: in vitro and in vivo evaluation

摘要

Moxifloxacin hydrochloride is a fluoroquinolone anti-infective agent useful in the treatment of eye infection such as conjunctivitis, keratitis and keratoconjunctivitis. An attempt has been made in the present research to formulate ocular inserts of moxifloxacin hydrochloride to increase residence time and prolong drug release. The ocular inserts were prepared using gelatin (18% and 20%), a natural biodegradable polymer and glycerin (70 % w/w of dry polymer) as a plasticizer. The cross linking was done by dipping cut inserts (8 mm diameter) in 10% w/v solution of glutaraldehyde in isopropyl alcohol (5 mL) for four different time period of 15, 30, 45 and 60 minutes to retard the release of drug. The inserts were then evaluated for their physicochemical parameters like uniformity of thickness, weight, drug content, swelling index and surface pH. The in vitro drug release studies were carried out using a bi-chambered donor receptor compartment model. In vivo drug release was carried out using rabbits as animal models. Formulations MHF4 and MHF8, which showed prolonged in vitro drug release, were subjected to in vivo study. In vitro and in vivo correlation for formulation MHF8 was found to be strong and productive. The drug was found to be active against selected microorganisms as was proved by microbial efficacy studies. Formulation MHF8 was found promising, as it achieved the target of the present study.