Paclitaxel-lipid prodrug liposomes for improved drug delivery and breast carcinoma therapy

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外文摘要：Paclitaxel(PTX)is widely applied for the treatment of unresectable and metastasis breast carcinoma as well as other cancers,whereas its efficacy is always impeded by poor solubility.Liposomes are one kind of the most successful drug carriers which are capable of solubilizing PTX and improving patients'tol-erance owing to excellent biocompatibility and biodegradability.However,poor compatibility between PTX and liposomes compromises the stability,drug loading and anti-tumor capacity of liposomal for-mulations.To address this issue,three lipids with various chain lengths,namely,myristic acid(MA,14C),palmitic acid(PA,16C)and stearic acid(SA,18C),were conjugated to PTX via ester bonds and the synthe-sized prodrugs with high lipophilicity were further formulated into liposomes,respectively.All liposomes show high stability and drug loadings,as well as sustained drug release.The chain lengths of lipids are negatively correlated with drug release and enzymatic conversion rates,which further impact the phar-macokinetics,tumor accumulation,and anti-tumor efficacy of liposomal PTX.Neither rapid nor slow drug release facilitates high tumor accumulation as well as anti-tumor efficacy of PTX.Among all liposomes,PTX-PA-loaded liposomes show the longest circulation and highest tumor accumulation of PTX and exert the most potent anti-tumor capacities in vivo,owing to its moderate drug release and enzymatic conver-sion rate.Witnessing its superior safety,PTX-PA liposomes hold potential for further clinical translation.

外文关键词：

PaclitaxelLipidsProdrugsLiposomesDrug releaseChemotherapy

作者：

Xin Wu、Xinmei Chen、Xinyu Wang、Haisheng He、Jianming Chen、Wei Wu

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作者单位：

Key Laboratory of Smart Drug Delivery of MOE,School of Pharmacy,Fudan University,Shanghai 201203,China

Department of Pharmacy,Fujian University of Traditional Chinese Medicine,Fuzhou 350122,China

Shanghai Wei Er Lab,Shanghai 201707,China

Shanghai Skin Disease Hospital,Tongji University School of Medicine,Shanghai 200443,China

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基金：

国家自然科学基金国家自然科学基金Shanghai Science and Technology Project of Little GiantShanghai Qingpu District Industry-University-Research Cooperative Development Funding ProjectHigh-level Talents of Fujian University of Chinese Medicine

项目编号：

82273867820301071902HX766002022-7X2019006-Talents

出版年：

2024

DOI：

10.1016/j.cclet.2023.108756

中国化学快报(英文版)

中国化学会

中国化学快报(英文版)

CSTPCD

影响因子：0.771

ISSN：1001-8417

年,卷(期)：2024.35(2)

参考文献量39