The effect of poloxamer 188 on nanoparticle morphology, size, cancer cell uptake, and cytotoxicity

• Published in: Nanomedicine 2010-02, Vol.6 (1), p.170-178
• Main Authors: Yan, Fei, PhD, Zhang, Chao, PhD, Zheng, Yi, PhD, Mei, Lin, PhD, Tang, Lina, BS, Song, Cunxian, PhD, Sun, Hongfan, MD, Huang, Laiqiang, PhD
• Format: Article
• Language: English
• Subjects: Breast cancer; Calorimetry, Differential Scanning; Cell Death - drug effects; Cell Line, Tumor; Cell Survival - drug effects; Cell viability; Coumarins - metabolism; Docetaxel; Humans; Inhibitory Concentration 50; Internal Medicine; Lactic Acid - chemistry; Microscopy, Confocal; Nanoparticles; Nanoparticles - chemistry; Nanoparticles - ultrastructure; Neoplasms - metabolism; Neoplasms - pathology; Particle Size; Poloxamer - toxicity; Poloxamer 188; Polyglycolic Acid - chemistry; Polylactic Acid-Polyglycolic Acid Copolymer; Spectroscopy, Fourier Transform Infrared; Taxoids - pharmacology
• ISSN: 1549-9634; 1549-9642
• DOI: 10.1016/j.nano.2009.05.004

Abstract The aim of this work was to investigate the effect of triblock copolymer poloxamer 188 on nanoparticle morphology, size, cancer cell uptake, and cytotoxicity. Docetaxel-loaded nanoparticles were prepared by oil-in-water emulsion/solvent evaporation technique using biodegradable poly(lactic- co -glycolic acid) (PLGA) with or without addition of poloxamer 188, respectively. The resulting nanoparticles were found to be spherical with a rough and porous surface. The nanoparticles had an average size of around 200 nm with a narrow size distribution. The in vitro drug-release profile of both nanoparticle formulations showed a biphasic release pattern. An increased level of uptake of PLGA/poloxamer 188 nanoparticles in the docetaxel-resistant MCF-7 TAX30 human breast cancer cell line could be found in comparison with that of PLGA nanoparticles. In addition, the docetaxel-loaded PLGA/poloxamer 188 nanoparticles achieved a significantly higher level of cytotoxicity than that of docetaxel-loaded PLGA nanoparticles and Taxotere ( P < .05). In conclusion, the results showed advantages of docetaxel-loaded PLGA nanoparticles incorporated with poloxamer 188 compared with the nanoparticles without incorporation of poloxamer 188 in terms of sustainable release and efficacy in breast cancer chemotherapy. From the Clinical Editor The effects of poloxamer 188, a triblock copolymer were studied on nanoparticle morphology, size, cancer cell uptake and cytotoxicity. An increased level of uptake of PLGA/poloxamer 188 nanoparticles in resistant human breast cancer cell line was demonstrated, resulting in a significantly higher level of cytotoxicity.