Cellular uptake and radiosensitization of SR-2508 loaded PLGA nanoparticles |
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Authors: | Cheng Jin Ling Bai Hong Wu Zenghui Teng Guozhen Guo Jingyuan Chen |
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Institution: | (1) Department of Radiation Medicine, Fourth Military Medical University, Xi’an, 710032, China;(2) Department of Clinical Laboratories, Xi’an Gaoxin Hospital, Xi’an, 710075, China;(3) Department of Pharmacy, Fourth Military Medical University, Xi’an, 710032, China;(4) Department of Pharmacology, Fourth Military Medical University, Xi’an, 710032, China;(5) Department of Occupational and Environmental Health, Fourth Military Medical University, Xi’an, 710032, China; |
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Abstract: | SR-2508 (etanidazole), a hypoxic radiosensitizer, has potential applications in radiotherapy. The poly(d,l-lactide-co-glycolide)(PLGA) nanoparticles containing SR-2508 were prepared by w/o/w emulsification-solvent evaporation method.
The physicochemical characteristics of the nanoparticles (i.e. encapsulation efficiency, particle size distribution, morphology,
in vitro release) were studied. The cellular uptake of the nanoparticles for the two human tumor cell lines: human breast
carcinoma cells (MCF-7) and human carcinoma cervices cells (HeLa), was evaluated by fluorescence microscopy and transmission
electronic microscopy. Cell viability was measured by the ability of single cell to form colonies in vitro. The prepared nanoparticles
were spherical in shape with size between 90 nm and 190 nm. The encapsulation efficiency was 20.06%. The drug release pattern
exhibited an initial burst followed by a plateau for over 24 h. The cellular uptake of nanoparticles was observed. Co-culture
of MCF-7 and HeLa cells with SR-2508 loaded nanoparticles showed that released SR-2508 retained its bioactivity and effectively
sensitized two hypoxic tumor cell lines to radiation. The radiosensitization of SR-2508 loaded nanoparticles was more significant
than that of free drug. |
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