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Int. J. Mol. Sci. 2014, 15(3), 3373-3388; https://doi.org/10.3390/ijms15033373

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

1
State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China
2
Department of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE 68198, USA
3
College of Chemistry and Environment Protection Engineering, Southwest University for Nationalities, Chengdu 610041, Sichuan, China
These authors contributed equally to the work.
*
Author to whom correspondence should be addressed.
Received: 17 December 2013 / Revised: 23 January 2014 / Accepted: 6 February 2014 / Published: 25 February 2014
(This article belongs to the Special Issue Bioactive Nanoparticles 2014)
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Abstract

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. View Full-Text
Keywords: salidroside; lipid-shell and polymer-core nanoparticles (LPNPs); PLGA; antitumor salidroside; lipid-shell and polymer-core nanoparticles (LPNPs); PLGA; antitumor
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Fang, D.-L.; Chen, Y.; Xu, B.; Ren, K.; He, Z.-Y.; He, L.-L.; Lei, Y.; Fan, C.-M.; Song, X.-R. Development of Lipid-Shell and Polymer Core Nanoparticles with Water-Soluble Salidroside for Anti-Cancer Therapy. Int. J. Mol. Sci. 2014, 15, 3373-3388.

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