Preparation and In vitro / In vivo characterization of spray dried microsphere formulation encapsulating 4-chlorocurcumin

The objective of the present study was to prepare and characterize in vitro and in vivo performance of a sustained release microsphere formulation of 4-chlorocurcumin, a novel curcumin analogue. A spray dried technique with ethylcellulose as the polymer was used in the preparation of these microspheres. Microspheres were characterized for drug content, particle size and shape, in vitro drug release and the drug-polymer interaction. To assess in vivo performance, both pharmacokinetics and hepatoprotective activity were investigated. Results were compared with an equivalent i.v. solution. The microspheres of 4-chlorocurcumin with ethylcellulose were successfully prepared using a spray-dried technique. These microspheres were able to sustain the release of the drug both in vitro as well as in vivo. Microspheres offered better pharmacokinetic and hepatoprotective properties to the drug compared to its solution form.