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  • Title: The Effect of Lipid Composition on the Liposomal Delivery of Camptothecin Developed by Active Click Loading.
    Author: Xie L, Zhang Q, Zhu Q, Wang Y, Niu S, Zhang X, Huang Y, Li J, Liu X, Xue Z, Zhao X, Zheng Y.
    Journal: Mol Pharm; 2024 May 06; 21(5):2327-2339. PubMed ID: 38576375.
    Abstract:
    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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