机构：[1]School of Pharmacy, Key Laboratory of Sichuan Province for Specific Structure of Small Molecule Drugs, Chengdu Medical College, Chengdu 610083, China.[2]Shandong Institute for Food and Drug Control, Ji'nan 250101, China.[3]Department of Pharmacy, The First Affiliated Hospital of Chengdu Medical College, Clinical Medical College, Chengdu Medical College, Chengdu 610083, China.
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.
基金：
Disciplinary Construction
Innovation Team Foundation of Chengdu Medical College
(CMC-XK-2104), National Undergraduate Training Program
for Innovation and Entrepreneurship (S202213705074,
202213705027, 202313705002, 202313705007), and Graduate
Research Innovation Project (YCX2022-01-25, YCX2023-01-
31, YCX2023-01-36).
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2023]版：
大类|2 区医学
小类|2 区药学3 区医学：研究与实验
最新[2023]版：
大类|2 区医学
小类|2 区药学3 区医学：研究与实验
第一作者：
第一作者机构：[1]School of Pharmacy, Key Laboratory of Sichuan Province for Specific Structure of Small Molecule Drugs, Chengdu Medical College, Chengdu 610083, China.
共同第一作者：
通讯作者：
推荐引用方式(GB/T 7714)：
Xie Lei,Zhang Qian,Zhu Qian,et al.The Effect of Lipid Composition on the Liposomal Delivery of Camptothecin Developed by Active Click Loading[J].Molecular Pharmaceutics.2024,21(5):2327-2339.doi:10.1021/acs.molpharmaceut.3c01140.
APA：
Xie Lei,Zhang Qian,Zhu Qian,Wang Yang,Niu Shuijiao...&Zheng Yaxin.(2024).The Effect of Lipid Composition on the Liposomal Delivery of Camptothecin Developed by Active Click Loading.Molecular Pharmaceutics,21,(5)
MLA：
Xie Lei,et al."The Effect of Lipid Composition on the Liposomal Delivery of Camptothecin Developed by Active Click Loading".Molecular Pharmaceutics 21..5(2024):2327-2339
