Improved delivery of the natural anticancer drug tetrandrine
Abstract
The
study aims at designing a nanoparticle-based delivery system to improve
the efficacy of the natural compound tetrandrine against lung cancer.
Nanoparticles from poly(lactic-co-glycolic acid) (PLGA) were
prepared by the emulsion solvent diffusion method and characterized for
their physicochemical properties and drug-loading efficiency.
Furthermore, the cellular uptake and the anti-cancerous activity was
studied on A549 cell line. To investigate the surface properties and
uptake, three different stabilizers were used to analyze the effect on
size and zeta potential of nanoparticles as well as the effect on the
cellular uptake. Nanoparticles in the size range of 180–200 nm with
spherical shape were obtained with polyvinyl alcohol (PVA),
Pluronic-F127 (PF127) and didodecyldimethylammonium bromide (DMAB), 2%,
1% and 0.1%, respectively. An entrapment efficiency of 50–60% with a
loading of 1.5–2% was observed. In vitro release profile at pH 7.4 PBS
solution showed a consistent release over 168 h. All particle systems
showed an improved performance over the pure drug at the same drug
concentration. DMAB stabilized particles demonstrated the most
pronounced effect against A549 cells compared to pure drug while PVA
stabilized particles were least effective in terms of antitumor
activity.
Graphical abstract
Keywords
- Anti-cancer activity;
- PLGA;
- Cell uptake;
- Surface properties;
- Drug delivery
- Corresponding
author at: Pharmaceutics and Biopharmacy, Philipps-Universität Marburg,
Ketzerbach 63, D-35037 Marburg, Germany. Tel.:
+49 6421 282 5885; fax: +49 6421 282 7016.
Copyright © 2014 Elsevier B.V. All rights reserved.
