Oxidation-Responsive Polymer-Drug Conjugates with a Phenylboronic Ester   Linker

doi:10.1002/marc.201500349

CORC > 北京大学 > 化学与分子工程学院

	Oxidation-Responsive Polymer-Drug Conjugates with a Phenylboronic Ester Linker
	Qiu, Fang-Yi ; Zhang, Mei ; Ji, Ran ; Du, Fu-Sheng ; Li, Zi-Chen
刊名	MACROMOLECULAR RAPID COMMUNICATIONS
	2015
关键词	naproxen oxidation-responsive phenylboronic ester polymer-drug conjugates RAFT REACTIVE OXYGEN HYDROGEN-PEROXIDE BIOMEDICAL APPLICATIONS POLYPRODRUG AMPHIPHILES DELIVERY RELEASE PRODRUG ACID ASSEMBLIES TUMORS
DOI	10.1002/marc.201500349
英文摘要	Polymer-drug conjugates have attracted great interest as one category of various promising nanomedicines due to the advantages of high drug-loading capacity, negligible burst release, and improved pharmacokinetics as compared with the small molecular weight drugs or the polymeric delivery systems with physically encapsulated drugs. Herein, a new type of oxidation- responsive polymer-drug conjugates composed of a poly(ethylene glycol) (PEG) block and a hydrophobic polyacrylate block to which Naproxen is attached through a phenylboronic ester linker is reported. The amphiphilic block copolymers are synthesized through the reversible addition- fragmentation chain transfer polymerization of the Naproxen-containing acrylic monomer using a PEG chain transfer agent. In neutral aqueous buffer, the conjugates formed nanoparticles with diameters of approximate to 150-300 nm depending on the length of the hydrophobic segment. The dynamic covalent bond of the phenylboronic ester is stabilized due to the hydrophobic microenvironment inside the nanoparticles. Upon exposure to H2O2, the phenylboronic ester is oxidized rapidly into the phenol derivative which underwent a 1,6-elimination reaction, releasing the intact Naproxen. The rate of drug release is influenced by the concentration of H2O2 and the hydrophobic block length. This type of oxidation-responsive polymer-drug conjugate is feasible for other drugs containing hydroxyl group or amino group.; National Natural Science Foundation of China [21474001]; National Science Fund for Distinguished Young Scholars of China [21225416]; SCI(E); ARTICLE; fsdu@pku.edu.cn; zcli@pku.edu.cn; 22; 2012-2018; 36
语种	英语
内容类型	期刊论文
源URL	[http://ir.pku.edu.cn/handle/20.500.11897/439275]
专题	化学与分子工程学院
推荐引用方式 GB/T 7714	Qiu, Fang-Yi,Zhang, Mei,Ji, Ran,et al. Oxidation-Responsive Polymer-Drug Conjugates with a Phenylboronic Ester Linker[J]. MACROMOLECULAR RAPID COMMUNICATIONS,2015.
APA	Qiu, Fang-Yi,Zhang, Mei,Ji, Ran,Du, Fu-Sheng,&Li, Zi-Chen.(2015).Oxidation-Responsive Polymer-Drug Conjugates with a Phenylboronic Ester Linker.MACROMOLECULAR RAPID COMMUNICATIONS.
MLA	Qiu, Fang-Yi,et al."Oxidation-Responsive Polymer-Drug Conjugates with a Phenylboronic Ester Linker".MACROMOLECULAR RAPID COMMUNICATIONS (2015).