Self-Assembly of an Amphiphilic Janus Camptothecin-Floxuridine Conjugate   into Liposome-Like Nanocapsules for More Efficacious Combination   Chemotherapy in Cancer

doi:10.1002/adma.201703135

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	Self-Assembly of an Amphiphilic Janus Camptothecin-Floxuridine Conjugate into Liposome-Like Nanocapsules for More Efficacious Combination Chemotherapy in Cancer
	Liang, Xiaolong ; Gao, Chuang ; Cui, Ligang ; Wang, Shumin ; Wang, Jinrui ; Dai, Zhifei
刊名	ADVANCED MATERIALS
	2017
关键词	cancer chemotherapy coordinated release drug-drug conjugates Janus nanoparticles self-assembly STEALTH LIPOSOMES DRUG-DELIVERY IN-VIVO THERAPY TUMOR NANOPARTICLES IRINOTECAN NANODRUG RATIOS
DOI	10.1002/adma.201703135
英文摘要	The combination of camptothecin (CPT) and fluoropyrimidine derivatives acts synergistically at a 1:1 molar ratio. Practically, the greatest challenge is the development of a single liposomal formulation that can both encapsulate and maintain this drug combination at an exact 1:1 ratio to achieve coordinated pharmacokinetics. Consequently, a new type of liposome-like nanocapsule (NC) is developed from a highly symmetric Janus camptothecin-floxuridine conjugate (JCFC) amphiphile, which is synthesized by coupling two hydrophobic CPT molecules and two hydrophilic floxuridine (FUDR) molecules to multivalent pentaerythritol via a hydrolyzable ester linkage. JCFC NCs possess remarkably high drug-loading contents, and no premature release because of the highly stable co-delivery of the drug combination without the need for any carrier. It is shown that JCFC NCs consistently provide synergy and avoid antagonism in a broad panel of tumor cell lines. In vivo delivery of JCFC NCs leads to longer blood retention half-life, higher tumorous accumulation and cellular uptake of drugs, and greatly enhanced efficacy in murine tumor models compared to CPT, FUDR, and CPT + FUDR. This liposomal strategy can be extended to other hydrophilic and hydrophobic anticancer drugs that are coupled to pentaerythritol to self-assemble into nanocapsules for drug self-delivery, pointing to potential clinical translation in near future.; National Key Research and Development Program of China [2016YFA0201400]; State Key Program of National Natural Science of China [81230036]; National Natural Science Foundation of China [81571810, 81371580]; Peking University Third Hospital [BYSY2015023]; Foundation for Innovative Research Groups of the National Natural Science Foundation of China [81421004]; SCI(E); ARTICLE; 40; 29
语种	英语
内容类型	期刊论文
源URL	[http://ir.pku.edu.cn/handle/20.500.11897/484593]
专题	工学院
推荐引用方式 GB/T 7714	Liang, Xiaolong,Gao, Chuang,Cui, Ligang,et al. Self-Assembly of an Amphiphilic Janus Camptothecin-Floxuridine Conjugate into Liposome-Like Nanocapsules for More Efficacious Combination Chemotherapy in Cancer[J]. ADVANCED MATERIALS,2017.
APA	Liang, Xiaolong,Gao, Chuang,Cui, Ligang,Wang, Shumin,Wang, Jinrui,&Dai, Zhifei.(2017).Self-Assembly of an Amphiphilic Janus Camptothecin-Floxuridine Conjugate into Liposome-Like Nanocapsules for More Efficacious Combination Chemotherapy in Cancer.ADVANCED MATERIALS.
MLA	Liang, Xiaolong,et al."Self-Assembly of an Amphiphilic Janus Camptothecin-Floxuridine Conjugate into Liposome-Like Nanocapsules for More Efficacious Combination Chemotherapy in Cancer".ADVANCED MATERIALS (2017).