Novel pH-Sensitive Micelles Generated by Star-Shape Copolymers Containing Zwitterionic Sulfobetaine for Efficient Cellular Internalization
作者：Jun Cao, Shuying Zhai, Chenlong Li, Bin He*, Yusi Lai, Yuanwei Chen, Xianglin Luo?, and Zhongwei Gu*
關鍵字：pH-Sensitive Micelles
論文來源：期刊
具體來源：Journal of Biomedical Nanotechnology, 2013, 9:1847-61
發(fā)表時間：2013年
pH-sensitive micelles are considered promising carriers for tumor targeted drug delivery. In this study, novel pH-sensitive star-shape copolymers of amphiphilic poly(
ε-caprolactone)-b-poly(N,N-diethylaminoethyl methacrylate)-r-poly(N-(3-sulfopropyl)-N-methacryloxyethy-N,N-diethylammoniumbetaine) (4sPCLDEAS) are designed and synthesized with the combination of ring opening polymerization (ROP) and atom radical transferpolymerization (ATRP). The structure of the copolymers is characterized by proton nuclear magnetic resonance spectra (
1H NMR). The poly(N-(3-sulfopropyl)-Nmethacryloxyethy-N,N-diethylammoniumbetaine) segment is used instead of poly(ethylene glycol) (PEG) as hydrophilic block in the copolymers to form polymeric micelles. The micelles present spherical shape, narrow size distribution, and are reponsive to the acidity. The CMC of the micelles is as low as 1×10
-3 mg.mL
?1. Doxorubin (DOX) is efficiently encapsulated in the micelles and the drug release is pH dependant. The cytotoxicity as well as the intracellular drug delivery of the micelles are investigated. The micelles are nontoxic to human cervical carcinoma (Hela) cells. The DOX loaded micelles are internalized in Hela cells efficiently, which are better than that of hydrophilic doxorubicin hydrochloride (DOX· HCl). These pH-sensitive micelles are potential promising carriers for anti-cancer drug delivery.