Stereocomplexation Assisted Assembly of Poly(γ-glutamic Acid)-graft-polylactide Nano-micelles and Their Efficacy as Anticancer Drug Carrier

Title:Stereocomplexation Assisted Assembly of Poly(γ-glutamic Acid)-graft-polylactide Nano-micelles and Their Efficacy as Anticancer Drug Carrier

Volume: 18 Issue: 2

Author(s): Shulin Dai, Yucheng Feng, Shuyi Li, Yuxiao Chen, Meiqing Liu, Chao Zhang*, Wei Zhang*Yihua Yin*

Affiliation:

• Guangdong Provincial Key Laboratory of Sensor Technology and Biomedical Instruments, School of Engineering, Sun Yat-Sen University, Guangzhou, 510006,China

• Department of Outpatient, The First Affiliated Hospital, Sun Yat-sen University, Guangzhou, 510080,China

• School of Chemistry, Chemical Engineering and Life Sciences, Wuhan University of Technology, Wuhan, Hubei, 430070,China

Keywords: Poly(lactic acid), poly(γ-glutamic acid), stereocomplexation, micelle, doxorubicin, anti-cancer drug carrier.

Abstract: Background: Micelles as drug carriers are characterized by their inherent instability due to the weak physical interactions that facilitate the self-assembly of amphiphilic block copolymers. As one of the strong physical interactions, the stereocomplexation between the equal molar of enantiomeric polylactides, i.e., the poly(L-lactide) (PLLA) and poly(D-lactide) (PDLA), may be harnessed to obtain micelles with enhanced stability and drug loading capacity and consequent sustained release.

Aims/Methods: In this paper, stereocomplexed micelles gama-PGA-g-PLA micelles) were fabricated from the stereocomplexation between poly(gama-glutamic acid)-graft-PLLA gama-PGA-g-PLA) and poly(gamaglutamic acid)-graft-PDLA gama-PGA-g-PLA). These stereocomplexed micelles exhibited a lower CMC than the corresponding enantiomeric micelles.

Result: Furthermore, they showed higher drug loading content and drug loading efficiency in addition to more sustained drug release profile in vitro. In vivo imaging confirmed that the DiR-encapsulated stereocomplexed gama-PGA-g-PLA micelles can deliver anti-cancer drug to tumors with enhanced tissue penetration. Overall, gama-PGA-g-PLA micelles exhibited greater anti-cancer effects as compared with the free drug and the stereocomplexation may be a promising strategy for fabrication of anti-cancer drug carriers with significantly enhanced efficacy.

Cite this article as:

Dai Shulin, Feng Yucheng, Li Shuyi, Chen Yuxiao, Liu Meiqing, Zhang Chao*, Zhang Wei*, Yin Yihua*, Stereocomplexation Assisted Assembly of Poly(γ-glutamic Acid)-graft-polylactide Nano-micelles and Their Efficacy as Anticancer Drug Carrier, Anti-Cancer Agents in Medicinal Chemistry 2018; 18 (2) . https://dx.doi.org/10.2174/1871520617666170911170104