1: J Control Release. 2009 Jan 5;133(1):11-7. Epub 2008 Oct 9.

Paclitaxel-loaded PEGylated PLGA-based nanoparticles: in vitro and in vivo
evaluation.

Danhier F, Lecouturier N, Vroman B, Jérôme C, Marchand-Brynaert J, Feron O, Préat
V.

Université Catholique de Louvain, Unité de Pharmacie Galénique, Avenue Mounier,
73-20, 1200 Brussels, Belgium.

The purpose of this study was to develop Cremophor EL-free nanoparticles loaded
with Paclitaxel (PTX), intended to be intravenously administered, able to improve
the therapeutic index of the drug and devoid of the adverse effects of Cremophor 
EL. PTX-loaded PEGylated PLGA-based were prepared by simple emulsion and
nanoprecipitation. The incorporation efficiency of PTX was higher with the
nanoprecipitation technique. The release behavior of PTX exhibited a biphasic
pattern characterized by an initial burst release followed by a slower and
continuous release. The in vitro anti-tumoral activity was assessed using the
Human Cervix Carcinoma cells (HeLa) by the MTT test and was compared to the
commercial formulation Taxol and to Cremophor EL. When exposed to 25 microg/ml of
PTX, the cell viability was lower for PTX-loaded nanoparticles than for Taxol
(IC(50) 5.5 vs 15.5 microg/ml). Flow cytometry studies showed that the cellular
uptake of PTX-loaded nanoparticles was concentration and time dependent. Exposure
of HeLa cells to Taxol and PTX-loaded nanoparticles induced the same percentage
of apoptotic cells. PTX-loaded nanoparticles showed greater tumor growth
inhibition effect in vivo on TLT tumor, compared with Taxol. Therefore,
PTX-loaded nanoparticles may be considered as an effective anticancer drug
delivery system for cancer chemotherapy.


PMID: 18950666 [PubMed - indexed for MEDLINE]

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