Amphiphilic diblock copolymers based on poly(2-ethyl-2-oxazoline) and poly(4-substituted-ε-caprolactone): Synthesis, characterization, and cellular uptake

Kang Yu Peng, Shiu Wei Wang, Ren Shen Lee*

*此作品的通信作者

研究成果: 期刊稿件文章同行評審

18 引文 斯高帕斯(Scopus)

摘要

Amphiphilic diblock copolymers with various block compositions were synthesized on poly(2-ethyl-2-oxazoline) (PEtOz) as a hydrophilic block and poly(4-methyl-ε-caprolactone) (PMCL) or poly(4-phenyl-ε-caprolactone) (PBCL) as a hydrophobic block. These PEtOz-b-PMCL and PEtOz-b-PBCL copolymers consisting of soft domains of amorphous PEtOz and PM(B)CL had no melting endothermal peaks but displayed Tg. The lower critical solution temperature (LCST) values for the PEtOz-b-PMCL, and the PEtOz-b-PBCL aqueous solution were observed to shift to lower temperature than PEtOz homopolymers. Their aqueous solutions were characterized using fluorescence techniques and dynamic light scattering (DLS). The block copolymers formed micelles with critical micelle concentrations (CMCs) in the range 0.6-11.1 mg L-1 in an aqueous phase. As the length of the hydrophobic PMCL or PBCL blocks elongated, lower CMC values were generated. The mean diameters of the micelles were between 127 and 318 nm, with PDI in the range of 0.06-0.21, suggesting nearly monodisperse size distributions. The drug entrapment efficiency and drug-loading content of micelles depend on block polymer compositions. In vitro cell viability assay showed that PEtOz-b-PMCL has low cytotoxicity. Doxorubicin hydrochloride (DOX)-loaded micelles facilitated human cervical cancer (HeLa) cell uptake of DOX; uptake was completed within 2 h, and DOX was able to reach intracellular compartments and enter the nuclei by endocytosis.

原文英語
頁(從 - 到)2769-2781
頁數13
期刊Journal of Polymer Science, Part A: Polymer Chemistry
51
發行號13
DOIs
出版狀態已出版 - 01 07 2013

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