诺氟沙星-壳聚糖微球的制备及释药性能

Preparation of norfloxacin-chitosan microsphere and its drug release property

利用乳液-化学交联法,用水溶性壳聚糖(CS)与诺氟沙星(NFX)制备诺氟沙星-壳聚糖微球(NFX-CSM)。根据正交实验设计,考察投料比、交联剂用量、转速和反应温度对质量指标的影响,选出最佳制备工艺条件;利用扫描电镜,红外光谱和Zeta电位仪对载药微球进行表征;用药物溶出度仪检测NFX-CSM在不同pH值环境下的释药速率,并考察不同交联剂用量和投料比((m(CS)-m(NFX))所制备的载药微球对释药速率的影响;将大肠杆菌与NFX-CSM共培养,检测载药微球的抗菌效果。研究结果表明:在最佳制备工艺条件下,制得载药微球的平均粒径约为4μm,球形圆整,分散性好,载药量和包封率分别为4.9%和42.3%;载药微球在不同pH值环境下均对药物有良好的缓释效果,其释药速率随交联剂用量的增加和投料比的增大而变小;NFX在CSM的协同抗菌作用下,抗菌效果明显增强。

Norfloxacin（NFX）-chitosan（CS） microsphere（NFX-CSM） was prepared by using water-soluble CS and NFX with emulsification and cross-linking process. Orthogonal design based on 4 factors： the feed ratio of CS to NFX, dosage of crosslinker, stirring speed and temperature, was studied to determine the optimum preparing technique of microsphere. NFX-CSM was characterized via scanning electron microscope, Fourier transform infrared spectrometer and Zeta potential measurement. The release speed of NFX was determined under different pH conditions with the dissolution apparatus. Effects of dosage of crosslinker and feed ratio of CS to NFX on drug release were examined. Antibacterial property was tested while E. coli and NFX-CSM were co-cultured. The results show that NFX-CSM has good shape and dispersibility with the average particle size of about 4μm; the drug loading and drug encapsulation efficiency of NFX-CSM are 4.9% and 42.3%, respectively; the sustained release is remarkable under different pH conditions; the drug release speed is decreased with the increase of feed ratio of CS to NFX and dosage of crosslinker. The antibacterial effect of NFX is improved obviously in the synergetic action of CS microsphere.