Study on doxoru bicin-loaded star-shaped multi-arm PLGA-PEG-NH2 nanomicelles
10.3760/cma.j.issn.1673-4181.2012.03.005
- VernacularTitle:载阿霉素星型多臂PLGA-PEG嵌段共聚物纳米胶束的构建
- Author:
Minmin CHEN
;
Shunxin ZHAO
;
Xu JIN
;
Cunxian SONG
;
Zhengpu ZHANG
;
Guilei MA
- Publication Type:Journal Article
- Keywords:
Doxorubicin;
Polymeric nanomicelles;
Star-shaped multi-arm PLGA-PEG;
Amphiphilic block copolymer
- From:
International Journal of Biomedical Engineering
2012;35(3):146-150,后插2
- CountryChina
- Language:Chinese
-
Abstract:
ObjectiveTo develop doxorubicine-loaded nanomicelles based on a type of novel starshaped 4-arm PLGA-PEG-NH2 amphiphilic block copolymers.Methods 4s-(PLGA-PEG-NH2) synthesized by 4s-PLGA and (H2N-PEG-NH2) according to N,N'-dicyclohexylcarbodiimide(DCC) condensation reaction was demonstrated by 1H NMR spectroscopy and gel permeation chromatography(GPC); DOX-loaded 4s-(PLGA-PEG-NH2) nanomicelles were self-assembled by doxorubicin(DOX) and 4s-(PLGA-PEG-NH2) via emulsion-solvent evaporation method and characterized in terms of morphology,particle size and size distribution,drug loading,encapsulation efficacy,cell uptake and cytotoxicity studies.Results4s-(PLGA-PEG-NH2) were capable of selfassembling intocore-shell nanomicelles structure and encapsulating DOX into their hydrophobic cores.The mean size of DOX-loaded 4s-(PLGA-PEG-NH2) was nanometer size; drug loading and encapsulation efficacy were around 7.5％ and 75.2％,respectively.Mean surface charge of the micelles was around -17.6 mV.In vitro cell uptake and cytotoxicity studies indicated that comparing to the DOX-loaded linear-(PLGA-PEG-PLGA)nanomicelles,DOX-loaded 4s-(PLGA-PEG-NH2) nanomicelles showed better performance in uptaking by HeLa cells and higher cytotoxicity to cancer cells.Conclusion4s-(PLGA-PEG-NH2) amphiphilic block copolymers can be successfully used in encapsulating DOX,self-assemblingcore-shell nanomicelles in aqueous solvent.Therefore,4s-(PLGA-PEG-NH2) copolymers can be considered as a promising drug carrier in effectively carrying hydrophobic drug,improving the efficacy while reducing the side effect.
