摘要
目的制备两性霉素B脂质复合物及胆固醇-聚乙二醇(PEG)修饰的两性霉素B脂质复合物并对其包封率和药动学进行研究。方法采用薄膜蒸发法制备两性霉素B脂质复合物及胆固醇-PEG修饰的两性霉素B脂质复合物,用动态光散射法测定粒径,采用Ultrafree-CL离心超滤管分离游离两性霉素B(F-AMB)与复合两性霉素B(L-AMB)检测包封率,用Wistar大鼠进行药动学研究。结果两性霉素B脂质复合物平均粒径为(115±20)nm;包封率大于99.9%;大鼠静脉注射,胆固醇-PEG修饰的两性霉素B脂质复合物ρ_(max)和AUC明显提高。结论采用薄膜蒸发法制备两性霉素B脂质复合物具有较高包封率,胆固醇-PEG修饰的两性霉素B脂质复合物能够延长体内循环时间。
OBJECTIVE To prepare cholesterol-PEG-modified amphotericin B liposomes and amphotericin B liposomes, and e- valuate their encapsulation efficiency and pharmacokinetics. METHODS It was employed to prepare both kinds of liposomes with the film-evaporation, the dynamic light scattering techniques and Ultrafree-CL were used to determine the mean diameter and the encapsu- lation efficiency~ respectively. Pharmaeokinetics was evaluated in Wista rats. RESULTS Mean diameter of the liposomes was （115 ＋ 20） nm, and the encapsulation efficiency was over 99.9%. Moreover, the pharmacokinetie study in rats indicated that choles- terol-PEG-modified liposomes could significantly increase the Pmax and AUC. CONCLUSION Amphotericin B liposomes prepared by film-evaporation method have high encapsulation efficiency, and cholesterol-PEG modification can prolong the circulation time of am- photericin B in vivo.
作者
修宪
冯彩霞
白晶
陈东健
赵伟
李晨晓
张兰
XIU Xian;FENG Cai-xia;BAI Jing;CHEN Dong-jian;ZHAO Wei;LI Chen-xiao;ZANG Lan(The Second Hospital of Shijiazhuang, Shijiazhuang 050051, China;CSPC Zhongqi Pharmaceutical Technology （Shijiazhuang） Co. , Ltd. , Shijiazhuang 050035, China;State Key Lab of Novel Pharmaceutical Preparations and Excipients ,Shijiazhuang 050035, Chi- na;The Fifth Hospital of Shijiazhuang , Shijiazhnang 050024, China)
出处
《中国药学杂志》
CAS
CSCD
北大核心
2018年第5期371-374,共4页
Chinese Pharmaceutical Journal
基金
科技部“十二五”重大新药创制项目资助(2014ZX09507001)
石家庄市科技支撑计划资助(171461293)
