脂质体
喜树碱
化学
药理学
药物输送
体内
药代动力学
药品
治疗指标
生物化学
色谱法
生物物理学
有机化学
医学
生物
生物技术
作者
Lei Xie,Qian Zhang,Qian Zhu,Yan Wang,Shuijiao Niu,Xinyue Zhang,Yuting Huang,Jiayao Li,Xiaoxue Liu,Xue Zhang,Xin Zhao,Yaxin Zheng
标识
DOI:10.1021/acs.molpharmaceut.3c01140
摘要
In the present study, we investigated the role of lipid composition of camptothecin (CPT)-loaded liposomes (CPT-Lips) to adjust their residence time, drug distribution, and therefore the toxicities and antitumor activity. The CPT was loaded into liposomes using a click drug loading method, which utilized liposomes preloaded with GSH and then exposed to CPT-maleimide. The method produced CPT-Lips with a high encapsulation efficiency (>95%) and sustained drug release. It is shown that the residence times of CPT-Lips in the body were highly dependent on lipid compositions with an order of non-PEGylated liposomes of unsaturated lipids < non-PEGylated liposomes of saturated lipids < PEGylated liposomes of saturated lipids. Interestingly, the fast clearance of CPT-Lips resulted in significantly decreased toxicities but did not cause a significant decrease in their in vivo antitumor activity. These results suggested that the lipid composition could effectively adjust the residence time of CPT-Lips in the body and further optimize their therapeutic index, which would guide the development of a liposomal formulation of CPT.
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