桉叶油羟丙基-β-环糊精包合物-原位凝胶复合系统的制备与评价

Study on Eucalyptus Oil Hydroxypropyl Cellulose β-Cyclodextrin Inclusion Compound/In Situ Gel Combination Delivery System

目的制备桉叶油羟丙基-β-环糊精包合物原位凝胶复合给药系统,提高桉叶油的水溶解度,同时达到滞留病灶部位且缓慢释放的效果。方法采用水溶液搅拌法制备桉叶油羟丙基-β-环糊精包合物,以海藻酸钠制备空白离子敏感型原位凝胶,将两者结合后对复合给药系统的体外溶蚀及体内滞留性进行评价。结果桉叶油羟丙基-β-环糊精包合物的含油率为(6.45±0.16)%,包合率(77.42±1.78)%。体外溶蚀实验表明,包合物原位凝胶复合系统的平均溶蚀率为(44.62±2.07)mg.cm 2.h 1。体外溶蚀实验结果表明,复合系统在24 h溶蚀完全;荧光活体成像系统检测体内滞留性实验结果表明,复合系统可在裸鼠肺部滞留12 h以上。结论桉叶油羟丙基-β-环糊精包合物原位凝胶复合系统可达到局部滞留并缓慢释放药物的目的。

OBJECTIVE To prepare hydroxypropyl cellulose-β-cyclodextrin （HP-β-CD） inclusion compound combined with sodium alginate in situ gel combination delivery system. And to improve the stability and water solubility of eucalyptus oil, which is a kind of volatile oil extracted from eucalyptus leaves, as well as to retain the drug in lungs of mice and to release it slowly. METHODS The method of agitation in water solution was applied to prepare HP-β-CD inclusion compound of eucalyptus oil, and sodium alginate was used to prepare ion-sensitive in situ gel. The combination delivery system obtained by adding the inclusion compound to the in situ gel followed by physically mixing. The combination delivery system＇s in vitro cumulative erosion rate and the retention property at lungs of Nu/Nu mice was examined. RESULTS The drug-loading rate of HP-β-CD inclusion compound was （6.45±0.16）%; the rate of inclusion was （77.42±1.78）%; the erosion rate of HP-β-CD inclusion-in situ gel combination delivery system was （44.62±2.07）mg·cm-2·h-1. In vitro erosion results showed that the delivery system eroded completely in 24 h. In vivo fluorescent image results demonstrated that the delivery system was able to retain in lungs for 12 h. CONCLUSION The combination delivery system can effectively retain at lungs of mice and slowly release drug.