CHEN Juan1��2�� HU Quan1�� HOU Zhen-qing1�� ZHANG Qi-qing1*
1. Research Center of Biomedical Engineering�� Xiamen University��Xiamen 361005�� China��2. Zhongshan Hospital�� Xiamen University��Xiamen 361004�� China
Abstract��
OBJECTIVE To prepare chitosan nanoparticle with controllable size and investigate its applications to targeting and sustained drug delivery system. METHODS The combination of an ion-induced and chemical crosslinking method was used to prepare chitosan nanoparticles�� and mitomycin C�� PEG and folic acid were bound covalently on the surface of chitosan nanoparticles in the presence of 1-ethyl-3-(3-dimethyllaminopropyl) carbodiimide hydrochloride (EDC)�� respectively. In vitro drug release test was carried out in different pH PBS solution. Confocal laser scanning microscope of Hela cell and in vivo imaging test were carried out using PEG and folic acid-modified chitosan nanoparticles labeled by Rhodamine B. RESULTS The diameter was in the range of 200 and 500 nm�� the drug-loading capability and entrapment efficiency were 25% and 50% ��respectively. The drug release was somewhat biphasic with an initial burst effect�� followed by a subsequent slower release. Furthermore�� increasing pH of the medium resulted in a faster release rate. Blank chitosan nanoparticles�� folic acid modified and both folic acid and PEG-modified nanoparticles were effectively uptaken by Hela cells�� while the single PEG-modified nanoparticles rarely entered the cell. By live imaging techniques�� folic acid-modified nanoparticles had a clear targeting character. While�� the PEG-modified chitosan nanoparticles enhanced circulation time in the bloodstream of mice. CONCLUSION By the method of ion-induced combined with chemical crosslinking�� steady chitosan nanoparticles with controlable size were obtained and suitable for active targeting drug delivery.
.Preparation of Chitosan Nanoparticles for Targeting and Sustained Drug Delivery System by Ion-induced Combined with Chemical Crosslinking[J] Chinese Pharmaceutical Journal, 2010,V45(18): 1400-1403
2010, Vol. 45 
