Novel albendazole-chitosannanoparticles for intestinal absorption enhancement and hepatic targetingimprovement in rats
Yang Liu, Xiao-qing Wang,Wei-xin Ren,Yuan-lan chen, Yang Yu, Jian-kang Zhang, Dilimulati·Bawudong, Jun-peng Gu, Xiao-dong Xu, Xue-nong Zhang
Journal of Biomedical Materials Research Part B（二区，IF=2.147）2013 Mar 26. doi: 10.1002/jbm.b.32908. [Epub ahead of print]
To improve the treatment of helminthiasis, filariasis, and colorectal cancer, albendazole-associated chitosan nanoparticles (ABZ-CS-NPs) were prepared using the emulsion crosslinking technique. Sodium tripolyphosphate and Poloxamer188 were used as the cross-linking agent and auxiliary solvent, respectively.The structural characteristics of the NPs were determined by X-ray diffraction toanalyze CS–albendazole interaction. Through animal studies,the NPs were evaluated in terms of theirphysicochemical characteristics, drug release behavior,in vivopharmacokinetic parameters, and biodistribution.ABZ-loaded NPs with uniformly spherical particles (157.8 nm±2.82 nm) showed efficient drug loading, efficient encapsulation, and high physical stability. The drug release from ABZ-CS-NPs was extended over several periods. Kinetic models were then fitted to determine therelease mechanisms.ABZ and its metabolite,albendazole sulphoxide (ABZSX), were analyzed by reversed-phase high-performance liquid chromatography. For the analysis, rats were used with mebendazole as the internal standard. Compared with therelative bioavailabilityvalues of ABZsuspension groups, those of ABZ and ABZSX were 146.05% and 222.15%, respectively. In addition, the plasma concentration versus time curve is consistent with that of the two compartment models. Results indicate that the ABZ-loaded NPs are promising ABZ candidates for passive diffusion in the oral treatment of hydatid cysts in the liver.
