阿苯达唑-壳聚糖微球的制备及其质量指标的考察

目的:考察阿苯达唑-壳聚糖微球(ABZ-CS-MS)的载药量、包封率、表面形态及结果特性,以及微球在不同介质中的体外释放特性。方法:采用乳化-交联固化法,以液体石蜡为油相,Span-80为乳化剂,戊二醛为交联剂,壳聚糖(chitosan,CS)为载体,制备阿苯达唑-壳聚糖微球(ABZ-CS-MS);应用光学显微镜测量ABZ-CS-MS的的粒径大小及其分布;用扫描电镜(SEM)观察ABZ-CS-MS的表面形态;用红外光谱(fourier transform infraredspectrometer,FT-IR)、X-线粉末衍射法(X-ray power diffraction,X-RD)和差示扫描热量法(differential scanning calo-rimetry,DSC)检测ABZ-CS-MS的特性;用体外动态透析法测定ABZ-CS-MS在不同介质条件下的释药性能。结果:所制备的ABZ-CS-MS形态圆整,粒径分布较为均匀,平均粒径为(153±7)μm,载药量为(20.92±0.15)%,包封率为(25.37±0.22)%;ABZ-CS-MS分别在不同介质(0.1mol/L HCl液、PBS(pH=3.5)、PBS(pH=7.4)和0.9%氯化钠溶液)中的释放均遵循Weibull方程,其中在PBS(pH=3.5)中释放效果最佳。结论:该法制备的ABZ-CS-MS的质量与性能良好,具有较好的载药量,包封率高,形态圆整,缓释作用明显。

Studies on Preparation and Quality Evaluation of Albendazole Loaded-Chitosan Microspheres

Objective:To study the preparation technique of ABZ-CS-MS the encapsulation efficiency the drug-loading rate the average diameter and shape were investigated.Methods:albendazole-loaded chitosan microspheres for embolization were achieved by emulsification cross-linking process with liquid paraffin as oil phase chitosan as water phase Span-80 as emulsifier and glutaraldehyde as cross linking agent.The particle size and distribution of microspheres were analyzed by optical microscope and the surface characterization of the microspheres was identified with scanning electronic microscope(SEM).The interaction of the drug and the polymer was analyzed by Application of infrared spectroscopy(FT-IR) X-ray power diffraction(XRD) and differential scanning calorimetry(DSC).Results:The novel microspheres with a global shape and narrow distribution were prepared.The average diameter was about(153±7)μm the drug-Loading rate was(20.92±0.15)% and the encapsulation efficiency of microspheres was(25.37±0.22)%.The drug release behavior at 0.1 mol/L HCL phosphate buffered saline(pH=3.5) and phosphate buffered saline(pH=7.4) and physiological saline are all conformed weibull distribution model the best effect of which is in PBS(pH= 3.5).Conclusion:The technique was feasible and microspheres with high drug-Loading rate and evident effect of sustained drug release were prepared.The solubility property of the albendazole solid dispersions was increased obviously.