Abstract
Purpose: :
Drug delivery in ocular therapy has long been a challenge that is associated with poor bioavailability. Liposomes can potentially serve as carrier systems for sustained and controlled delivery of drugs, to overcome the current limitations. The aim of this work is to investigate the release of drug, ciprofloxacin hydrochloride from liposomes in an in vitro dialysis setup. Different parameters such as lipid acyl chains and source, cholesterol concentrations and pH of the release medium were studied
Methods: :
The drug, ciprofloxacin hydrochloride is routinely used in the treatment of external eye infections. Briefly, multilamellar vesicles (MLVs) with or without cholesterol inclusions, were prepared by ethanol injection method. Subsequent size reduction of MLVs to large unilamellar vesicles (LUVs) were carried out by extrusion technique. Ciprofloxacin hydrochloride was loaded into preformed liposomes (LUVs) by remote loading technique. The drug release was carried at 37°C against PBS buffer in an in-vitro dialysis setup.
Results: :
A concentration-dependent release behavior of ciprofloxacin hydrochloride from liposomes was observed. Liposomal formulations which contained an additive, cholesterol, demonstrated a sustained release for over a month. In comparison, the release from the liposomal formulations without cholesterol was found to be rapid (all drug released in 5 days). In addition, the release was independent of lipid acyl chain and source of the liposome. The release of the drug was however found to be dependent on the pH of the release medium, with a faster release at pH 9.0.
Conclusions: :
A sustained release formulation of ciprofloxacin hydrochloride in liposomes containing cholesterol was developed which could potentially be used for delivery of ophthalmic drugs such as antibiotics.
Keywords: antibiotics/antifungals/antiparasitics • lipids • pH