Self-Assembled Micelles from an Amphiphilic Hyperbranched Copolymer with Polyphosphate Arms for Drug Delivery
作者：Liu, J.Y.; Huang, W.*; Pang, Y.; Zhu, X.Y.; Zhou, Y. F.; Yan, D.Y.
關鍵字：Amphiphilic Hyperbranched Copolymer,Polyphosphate Arms,Drug Delivery
論文來源：期刊
具體來源：Langmuir 2010, 26, 10585. http://pubs.acs.org/doi/pdf/10.1021/la1006988
發(fā)表時間：2010年
A novel type of amphiphilic hyperbranched multiarm copolymer [H40-star-(PLA-b-PEP-OH)]
was synthesized through a two-step ring-opening polymerization (ROP)
procedure and applied to drug delivery. First, Boltorn H40 was used as
macroinitiator for the ROP of l-lactide to form the intermediate (H40-star-PLA-OH). Then, the ROP of ethyl ethylene phosphate was further initiated to produce H40-star-(PLA-b-PEP-OH). The resulting hyperbranched multiarm copolymers were characterized by 1H, 13C, and 31P NMR, GPC, and FTIR spectra. Benefiting from the amphiphilic structure, H40-star-(PLA-b-PEP-OH)
was able to self-assemble into micelles in water with an average
diameter of 130 nm. In vitro evaluation of these micelles demonstrated
their excellent biocompatibility and efficient cellular uptake by methyl
tetrazolium assay, flow cytometry, and confocal laser scanning
microscopy measurements. Doxorubicin-loaded micelles were investigated
for the proliferation inhibition of a Hela human cervical carcinoma cell
line, and the Doxorubicin dose required for 50% cellular growth
inhibition was found to be 1 μg/mL. These results indicate that H40-star-(PLA-b-PEP-OH) micelles can be used as safe, promising drug-delivery systems.