基于β-环糊精为骨架材料的茶树油微球制备、表征及体外释药研究  

Preparation,characterization and in vitro drug release of tea tree oil microspheres using β-cyclodextrin as framework material

作　　者：张寒[1] 张博 汪兴军 郑梦迪 申旭霁[1] 李伟泽[1] ZHANG Han;ZHANG Bo;WANG Xing-jun;ZHENG Meng-di;SHEN Xu-ji;LI Wei-zhe(Department of Pharmacy, Xi＇an Medical College, Xi ＇an 710021, China;Shanxi Bicong Pharmaceutical Group Holding Company Limited, Xi ＇an 710021, China)

机构地区：[1]西安医学院药学院,西安710021 [2]陕西必康制药集团有限公司,西安710021

出　　处：《国际药学研究杂志》2018年第2期144-149,共6页Journal of International Pharmaceutical Research

基　　金：陕西省科技厅面上项目(2017JM8109);西安医学院省级重点学科-药学(1007);西安医学院药学重点学科建设项目(2016YXXK01;2016YXXK07和2016YXXK21);西安医学院2016年博士科研启动基金(2016D0CO9)

摘　　要：目的以β-环糊精(β-CD)为骨架材料制备茶树油微球(TTO-β-CDPM),优化其制备工艺并进行药剂学性能考察,为茶树油提供一种新的应用形式。方法以微球产率、包油率为评价指标,通过正交实验筛选优化茶树油微球成型最佳工艺,通过红外(IR)、示差热扫描(DSC)和扫描电镜对微球进行表征,并考察TTO-β-CDPM的稳定性与体外释药行为特征。结果TTO-β-CDPM制备工艺最佳条件:茶树油与β-环糊精微球的比例为1∶8,包合温度为30℃,包合时间为1 h,β-环糊精微球与水比例为1∶10。在此条件下,制备TTO-β-CDPM的平均产率为(82.20±0.00)%,制得的TTO-β-CDPM对TTO的相对包封率为(58.50±0.00)%,而TTO-β-CDPM对TTO的绝对平均载油量为(8.15±2.23)%。IR、DSC结果均显示茶树油的特征峰在制成微球后消失,表明β-CD通过交联形成骨架型多孔状微球,能包载茶树油且相容性较好;扫描电镜结果也显示TTO-β-CDPM形成的球体结构规整,圆球成形较好,粘连少。经80℃水浴8 h后,TTO-β-CDPM的保留率为63.1%,是未包合的茶树油保留率的4.15倍,表明TTO-β-CDPM稳定性良好;恒温动态模拟释药8 h时,TTO-β-CDPM中茶树油释放量为19.52%,表明β-CD骨架微球对于茶树油具有显著的缓释作用。结论以β-CD为骨架材料,所制备的微球对于茶树油载药量高、稳定性好、缓释行为明显,因此,具有良好的应用前景和推广价值。Objective To prepare the tea tree oil（TTO）-loaded β-cyclodextrin（β-CD）polymerized microspheres（TTO-β-CDPM）using β-CD as a skeletal material,optimize the preparation process,and investigate the characteristics and properties of TTO-β-CDPM to provide a new application form of TTO. Methods The TTO-β-CDPM production rate and the TTO-loading rate were as index, the preparation process of TTO-β-CDPM was optimized by the orthogonal design method,and the prepared TTO-β-CDPM were characterized by the infrared（IR）spectroscopy,differential thermal scanning（DSC）and scanning electron microscopy（SEM）.Meanwhile,the stability and in vitro drug release of TTO-β-CDPM were also investigated. Results The optimal conditions for the TTO-β-CDPM preparation were as follows：TTO∶β-CDPM=1∶8,temperature 30℃,holding time 1 h,and β-CDPM：water = 1∶10.Under these conditions,the average yield of TTO-β-CDPM preparation was（82.20±0.00）% and the relative TTO-encapsulation rate of TTO-β-CDPM was（58.50±0.00）%,while the absolute average TTO-loading of the TTO-β-CDPM reached（8.15±2.23）%. The IR spectroscopy and DSC showed that the characteristic peaks of TTO disappeared in the TTO-β-CDPM,indicating that the β-CD formed a skeleton type multipore microspheres by crosslinking,which encapsulated the TTO with good compatibility. The SEM also verified the spherical structure of TTO-β-CDPM,which had the well sphericized form with little adhesion. After treatment at 80℃ for 8 hours in a water bath, the retention rate of TTO-β-CDPM was 63.1%,which was 4.15 times that of the unwrapped TTO,indicating the good stability of TTO-β-CDPM. In the drug-release test at 37℃ for 8 h,the release rate of TTO from TTO-β-CDPM was 19.52%. These data suggested that the β-CD skeletal microspheres likely exerted a significant slow-release effect on the release of TTO from TTO-β-CDPM. Conclusion The TTO-β-CDPM had higher TTO-loading,good stability and slow-release effect,showing a bright future of furthe

关 键 词：Β-环糊精 微球 茶树油 稳定性 缓释 

分 类 号：R94[医药卫生—药剂学]