阿苯达唑-壳聚糖微球的制备及其质量指标的考察  

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

作　　者：张光宇[1,2] 晏语[1] 倪进[1] 王晓青[1] 杨程[1] 张学农[1] 任伟新[2] 迪理木拉提.巴吾东 顾俊鹏[2] 许晓东[2] 

机构地区：[1]苏州大学医学部药学院,江苏苏州215123 [2]新疆医科大学附属第一医院,新疆乌鲁木齐830054

出　　处：《抗感染药学》2012年第2期108-114,共7页Anti-infection Pharmacy

基　　金：国家自然科学基金资助(编号:30690102);国家科技部十一五"重大新药创制"技术平台项目资助(编号:2009ZX09310-001)

摘　　要：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。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 identi- fied 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）um, 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.

关 键 词：阿苯达唑 壳聚糖 肝动脉栓塞 微球 制备 体外释放 

分 类 号：R927.11[医药卫生—药学]