Preparation, characterization, in vitro release, and pharmacokinetic studies of curcumin-loaded mPEG-PVL nanoparticles

Curcumin shows several pharmacological activities with low toxicity, but its low water solubility limits its usage. To overcome these drawback, methoxy poly(ethylene glycol)-b-poly (-valerolactone) was synthesized through ring-opening polymerization with mPEG and -valerolactone as raw materials and hydrochloride ethyl ether as catalyst. The nanoparticles were developed by thin-film hydration and used as the delivery system for curcumin. The pharmacokinetics, in vitro release and safety of curcumin-loaded nanoparticles were evaluated. The results showed that nanoparticles had high drug-loading capacity (11.70 %) and entrapment efficiency (92.66 %). The water solubility of curcumin was increased to 1.851 mg/mL, which was approximately 1.73 x 10(5) times higher than that of free curcumin. The plasma AUC(0-a) and V (z) of curcumin-loaded nanoparticles were 3.60- and 4.56-fold higher than that of curcumin control solution, respectively. The CLz of curcumin-loaded nanoparticles was decreased by 3.60-fold. The MRT0-a changed from 0.284 to 4.657 h. Hemolysis test results revealed that the mPEG-PVL was safe for intravenous injection. These results clearly showed that the curcumin-loaded nanoparticles were suitable to be a delivery vehicle for curcumin.