YANG Zi-ming;PENG Zheng;ZHOU Min;LI Si-dong;PANG Yu-xin;LI Hong;LI Pu wang
. 2013, 44(12): 1703-1707.
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A novel drug-loaded polymer chitosan microsphere with targeted and slow-release function was prepared using complex coacervation method, with folic acid targeted receptor modified chitosan as the carrier material and 5-fluorouracil as the model drug. The characteristics of the microspheres, including morphology structure, particle size and size distribution, embedding rate, drug loading, infrared spectrum and in vitro drug release properties, were investigated by fourier infrared spectrometer, scanning electron microscope, laser particle size analyzer, laser confocal microscope, ultraviolet spectrum and other modern instruments and analysis method. The results showed that the model drug was successfully embedded in the folic acid modified chitosan microspheres, with 86.5% embedding rate and 32.7% drug loading. The chitosan microspheres were in spherical with good dispersibility and diameter mostly around 5 μm. Laser confocal microscope results indicated that the microsphere was core-shell structure. In vitro drug release experiment showed chitosan drug-loaded microspheres had good slow release effect, with 70% and 40% release rate after 24 hours released in simulation of gastric juice (pH = 1.2) and simulation intestinal juice (pH = 7.4), respectively, which demonstrated the drug release rate was relevant to release medium pH value.