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KMID : 0369820150450070659
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Jorunal of Korean Pharmaceutical Sciences
2015 Volume.45 No. 7 p.659 ~ p.667
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Cellular uptake of poly(dl-lactide-co-glycolide) nanoparticles: effects of drugs and surface characteristics of nanoparticles
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Lee Sang-Seung
Lee Yong-Bok
Oh In-Joon
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Abstract
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In general, nanoparticles are internalized into cells by endocytosis. In the present study, we examine the cellular uptake of poly(lactic-co-glycolic) (PLGA) nanoparticles according to the hydrophilicity of the incorporated drug. Rhodamine B was used as a hydrophilic drug model and coumarin 6 as a hydrophobic drug model, both of which had fluorescent characteristics. The cellular uptake of the drug-loaded PLGA nanoparticles prepared by the solvent evaporation method was examined by flow cytometry and confocal microscopy. Rhodamine B could not pass through the membrane of HEK293 cells, however, rhodamine B-loaded PLGA nanoparticles could enter cells more easily. Conversely, both coumarin 6 and coumarin 6-loaded PLGA nanoparticles were observed inside cells, however, a higher fluorescence intensity was seen with coumarin 6-loaded PLGA nanoparticles in HEK293 cells than that of coumarin 6 alone. In order to investigate the nanoparticle uptake by cells, a fluorescent amine-PLGA (FA-PLGA), a PLGA polymer covalently bound directly to fluoresceinamine, was synthesized and observed inside cells by flow cytometry and confocal microscopy. The fluorescence of coumarin 6-loaded PLGA nanoparticles coated with chitosan was detected at the surface of cells, suggesting a charge interaction of the positive chitosan/PLGA nanoparticles with the negative cell membrane. This study presents the uptake of hydrophilic and hydrophobic nanoparticles in HEK293 cells.
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KEYWORD
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PLGA, Nanoparticles, Cellular uptake, Flow cytometry
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