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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 the eucalyptus oil hydroxypropyl-β-cyclodextrin inclusion complex in situ gel compound delivery system to improve the water solubility of eucalyptus oil, and to achieve the site of sustained lesion and slow release effect. Methods The inclusion compound of eucalyptus oil hydroxypropyl-β-cyclodextrin was prepared by stirring with aqueous solution and the blank ion-sensitive in situ gel was prepared by sodium alginate. In vivo retention was evaluated. Results The oil content of eucalyptus oil hydroxypropyl-β-cyclodextrin inclusion complex was (6.45 ± 0.16)%, the inclusion rate was (77.42 ± 1.78)%. In vitro dissolution experiments showed that the average dissolution rate of the in situ gel composite system was (44.62 ± 2.07) mg.cm2h1. The results of in vitro dissolution experiment showed that the composite system completely dissolved at 24 h. The fluorescence in vivo imaging system was used to detect the in vivo retention. The results showed that the composite system could stay in the lung of nude mice for more than 12 h. Conclusion Eucalyptus oil hydroxypropyl-β-cyclodextrin inclusion complex in situ gel system can achieve local retention and slow release of drugs.