Journal of Industrial and Engineering Chemistry, Vol.75, 115-122, July, 2019
Endocytosis of poly(ethylene sodium phosphate) by macrophages and effect of polymer length on cellular uptake
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Phosphorus-containing polymers are taking a growing interest as a bio-applicable material. Anionic poly (phosphodiester) is one type of phosphorus-containing polymer and has a similar backbone structure to teichoic acid (TA), which makes up the cell walls of gram-positive bacteria. In this study, we synthesized a copolymer of ethylene sodium phosphate and butynyl phosphate (P(EPㆍNa/BYP)), which mimics TA and, thus, should be taken up by macrophages by the same mechanism as bacterial cells. In-vitro studies showed that RAW 264.7 mammalian macrophages exhibited higher uptake of P(EPㆍNa/BYP) than L929 mammalian fibroblasts. Further, the uptake of P(EPㆍNa/BYP) by macrophages decreased in the presence of dextran sulfate; this implies that the scavenger receptor contributes to endocytosis of P(EPㆍNa/BYP). Invitro studies on P(EPㆍNa/BYP) with different lengths (38, 85, and 127 phosphate residues) showed that P (EPㆍNa/BYP) with 127 phosphate residues led to the highest intracellular transportation and the least gene expressions of IL-6 and TNF-α. These results demonstrate that water-soluble poly(phosphodiester) can be used as a modifier to deliver medical drugs to macrophages.
Keywords:Poly(phosphoester);Degradable polymer;Macrophages;Drug delivery system;Bioorthogonal labeling
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