Development of Lipid-Shell and Polymer Core Nanoparticles with Water-Soluble Salidroside for Anti-Cancer Therapy

International Journal of Molecular Sciences

Dai-Long Fang¹  Yan Chen¹  Bei Xu¹  Ke Ren³  Zhi-Yao He¹  Li-Li He²  Yi Lei¹  Chun-Mei Fan¹ 

[1]State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China

[2] E-Mails:

[3]College of Chemistry and Environment Protection Engineering, Southwest University for Nationalities, Chengdu 610041, Sichuan, China

[4] E-Mail:

[5]Department of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE 68198, USA

[6] E-Mail:

关键词: salidroside;    lipid-shell and polymer-core nanoparticles (LPNPs);    PLGA;    antitumor;   

DOI  :  10.3390/ijms15033373

来源: mdpi

【 摘 要 】

Salidroside (Sal) is a potent antitumor drug with high water-solubility. The clinic application of Sal in cancer therapy has been significantly restricted by poor oral absorption and low tumor cell uptake. To solve this problem, lipid-shell and polymer-core nanoparticles (Sal-LPNPs) loaded with Sal were developed by a double emulsification method. The processing parameters including the polymer types, organic phase, PVA types and amount were systemically investigated. The obtained optimal Sal-LPNPs, composed of PLGA-PEG-PLGA triblock copolymers and lipids, had high entrapment efficiency (65%), submicron size (150 nm) and negatively charged surface (−23 mV). DSC analysis demonstrated the successful encapsulation of Sal into LPNPs. The core-shell structure of Sal-LPNPs was verified by TEM. Sal released slowly from the LPNPs without apparent burst release. MTT assay revealed that 4T1 and PANC-1 cancer cell lines were sensitive to Sal treatment. Sal-LPNPs had significantly higher antitumor activities than free Sal in 4T1 and PANC-1 cells. The data indicate that LPNPs are a promising Sal vehicle for anti-cancer therapy and worthy of further investigation.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland