Tropical Journal of Pharmaceutical Research
Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria
Vol. 15, No. 7, 2016, pp. 1353-1360
Bioline Code: pr16179
Full paper language: English
Document type: Research Article
Document available free of charge
Tropical Journal of Pharmaceutical Research, Vol. 15, No. 7, 2016, pp. 1353-1360
© Copyright 2016 - Tropical Journal of Pharmaceutical Research
Development of docetaxel and alendronate-loaded chitosan-conjugated polylactide-co-glycolide nanoparticles: In vitro characterization in osteosarcoma cells|
Liu, Ya-Feng; Liu, Rui; Li, Xue-Yang; Song, Zhen & Zhao, Xue-Hang
Purpose: To develop docetaxel (DTX)- and alendronate (ALN)-loaded, chitosan (CS)-conjugated polylactide-
co-glycolide (PLGA) nanoparticles (NPs) to increase therapeutic efficacy in osteosarcoma cells.
Methods: Drug-loaded PLGA NPs were prepared by nanoprecipitation and chemically conjugated by
the carboxylic group of PLGA to the amine-bearing CS polymer. The nanocarrier was characterized by
dynamic light scattering, transmission electron microscopy, scanning electron microscopy, and
differential scanning calorimetry as well as by in vitro drug release and cell culture studies.
Results: NP size was within the tumour targeting range (~200 nm) with an effective positive charge (20
mV), thus increasing cellular uptake efficiency. Morphological analysis revealed clear spherical particles
with uniform dispersion. The NPs exhibited identical sustained release kinetics for both DTX and ALN.
CS-conjugated PLGA with dual-drug-loaded (DTX and AL) NPs showed typical time-dependent cellular
uptake and also displayed superior cytotoxicity in MG-63 cells compared with blank NPs, which were
safe and biocompatible.
Conclusion: Combined loading of DTX and ALN in NPs increased the therapeutic efficacy of the
formulation for osteosarcoma treatment, thus indicating the potential benefit of a combinatorial drug
regimen using nanocarriers for effective treatment of osteosarcoma.
Chitosan; Docetaxel; Alendronate; Nanocarriers; Sustained-release kinetics; Polylactide-coglycolide; Osteosarcoma; Cellular uptake
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