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Preparation, Characterization, and In Vitro Evaluation of Docetaxel-Loaded Poly(lactic acid)-Poly(ethylene glycol) Nanoparticles for Parenteral Drug Delivery

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The aim of this study was to develop a suitable drug delivery system without Tween 80 and design docetaxel (DTX)-loaded PLA-PEG nanoparticles to improve solubility and decrease side effect of docetaxel. DTX-loaded PLA-PEG nanoparticles were prepared by modified solvent volatilixation method and characterized by particle size distribution, zeta potential and entrapment efficiency. The morphology of DTX loaded PLA-PEG nanoparticles was approximately spherical. The mean diameter and zeta potential of freeze-dried PLA-PEG nanoparticles were 205 ± 8.1 nm and –24.17 ± 2.20 mV, respectively. The average entrapment efficiency and drug loading of freeze-dried DTX- loaded PLA-PEG nanoparticles were 91.83 ± 1.28% and 8.17 ± 0.35%, respectively. The in vitro release showed that the release from DTX loaded PLA-PEG nanoparticles was slower than from Duopafei® and followed the Weibull equation. Cytotoxicity of Duopafei® and DTX loaded PLAPEG nanoparticles was evaluated. Compared with Duopafei®, DTX-loaded PLA-PEG nanoparticles showed similar cytotoxicity against three human cancer cell lines and lower toxicity on human normal hepatocellular HL-7702 cells. The apoptosis was detected and measured with Hoechst 33342 and AnnexinV-FITC kit. Compared with Duopafei®, DTX-loaded PLA-PEG nanoparticles revealed similar cytotoxicity against A549 cells by inducing similar apoptosis. These results indicated that the PLA-PEG nanoparticles obtained in this study could potentially be exploited as a carrier without Tween 80, which improved drug solubility and decrease side effect of docetaxel.
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Keywords: APOPTOSIS; CYTOTOXICITY; DOCETAXEL; NANOPARTICLES; POLY(LACTIC ACID)-POLY(ETHYLENE GLYCOL) COPOLYMER (PLA-PEG)

Document Type: Research Article

Publication date: December 1, 2010

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  • Journal of Biomedical Nanotechnology (JBN) is a peer-reviewed multidisciplinary journal providing broad coverage in all research areas focused on the applications of nanotechnology in medicine, drug delivery systems, infectious disease, biomedical sciences, biotechnology, and all other related fields of life sciences.
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