Synthesis, self-assembly in water, and cytotoxicity of MPEG-block-PLLA/DX conjugates.
Docetaxel (DX) is one of the most effective antineoplastic drugs. Its current clinical administration is limited because of its hydrophobicity and serious side effects. A polymer/DX conjugate is designed and successfully prepared to solve these problems. It is monomethoxy-poly(ethylene glycol)-block-poly(L-lactide)/DX (MPEG-PLLA/DX). It was synthesized by reacting DX with carboxyl-terminated copolymer MPEG-PLLA, which was prepared by reacting succinic anhydride with hydroxyl-terminated copolymer monomethoxy-poly(ethylene glycol)-block-poly(L-lactide) (MPEG-PLLA). Its structure and molecular weight was confirmed by (1)H NMR and GPC. The MPEG-PLLA/DX micelles in aqueous solution were prepared using a solvent displacement method and characterized by dynamic light scattering for size and size distribution, and by transmission electron microscopy for surface morphology. Its antitumor activity against HeLa cancer cells evaluated by MTT assay showed that it had a similar antitumor activity to pure DX at the same drug content.
Xie
Zhigang
Z
State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, People's Republic of China.
Lu
Tiancheng
T
Chen
Xuesi
X
Zheng
Yonghui
Y
Jing
Xiabin
X
D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D000077143:Docetaxel; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D007773:Lactates; D008823:Micelles; D015394:Molecular Structure; D008970:Molecular Weight; D011092:Polyethylene Glycols; D011108:Polymers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D043823:Taxoids; D014867:Water
D000970:Antineoplastic Agents; D007773:Lactates; D008823:Micelles; D011108:Polymers; D043823:Taxoids; C088513:poly(lactic acid-ethylene glycol); D014867:Water; D000077143:Docetaxel; D011092:Polyethylene Glycols; C028210:monomethoxypolyethylene glycol