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Characterization and in-vitro bioactivity evaluation of paclitaxel-loaded polyester nanoparticles

López-Gasco, Patriciaa; Iglesias, Irenea; Benedí, Juanaa; Lozano, Rafaelb; Blanco, María Doloresc

doi: 10.1097/CAD.0b013e328355a6c6
Preclinical Reports

Paclitaxel, an antimicrotubular agent used in the treatment of ovarian and breast cancer, was encapsulated in nanoparticles of poly(DL-lactide-co-glycolide) and poly(ε-caprolactone) polymers using the double emulsion–solvent evaporation technique. The morphology, size distribution, drug encapsulation efficiency, thermal degradation and in-vitro drug release profile were characterized. High-performance liquid chromatography was used to determine the drug encapsulation efficiency and in-vitro drug release profile. MCF-7 breast cancer cells were used to evaluate the cytotoxicity (MTT assay), the cellular uptake and the cell cycle. The particle size was in the range of 200–400 nm. Poly(lactide-co-glycolide) nanoparticles showed more effective cellular uptake compared with those of poly(ε-caprolactone). Unloaded nanoparticles were found to be cytocompatible on MCF-7 cells and paclitaxel formulations showed efficacy in killing MCF-7 cells. Paclitaxel-loaded nanoparticles induced the release of the drug-blocking cells in the G2/M phase. Paclitaxel-loaded nanoparticles may be considered a promising drug delivery system in the evaluation of an in-vivo model.

Departments of aPharmacology

bInorganic and Bioinorganic, School of Pharmacy

cDepartment of Biochemistry and Molecular Biology, School of Medicine, Complutense University of Madrid, Madrid, Spain

Correspondence to María Dolores Blanco, PhD, Department of Biochemistry and Molecular Biology, School of Medicine, Complutense University of Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain Tel: +34 913 941 447; fax: +34 913 941 691; e-mail:

Received January 12, 2012

Accepted May 8, 2012

© 2012 Lippincott Williams & Wilkins, Inc.