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Drug Release Profile and Cellular Uptake of Polymeric Prodrugs Synthesized from Amphiphilic Blockcopolymer Using Mechanically Produced Macromonomers Possessing Anhydrate as a Terminal Group

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In this paper, the polymeric micelle was fabricated with amphiphilic block copolymer which was synthesized by the condensation of mechanochemically produced PBzMA macromonomer with a-methyl-w-aminopropoxy polyoxyethylene. Although the polymeric micelles containing 5-fluorouracil (5-FU) or rohdamine showed the narrow size distribution as well as blank polymeric micelles, the particle diameter of the polymeric micelles containing 5-FU or rohdamine was larger than that of blank polymeric micelle. Polymeric micelle containing 5-FU slowly released 5-FU and about 10 % of 5-FU was released within 72 h. The present polymeric micelle was uptaken by A549 cells, but HepG2 cells did not. Cytotoxicity of Polymeric micelle containing 5-FU was not observed against HepG2 and A549 cells in this experimental condition. It was considered that the slow release of 5-FU from Polymeric micelle might cause the insufficient cytotoxicity.
Title: Drug Release Profile and Cellular Uptake of Polymeric Prodrugs Synthesized from Amphiphilic Blockcopolymer Using Mechanically Produced Macromonomers Possessing Anhydrate as a Terminal Group
Description:
In this paper, the polymeric micelle was fabricated with amphiphilic block copolymer which was synthesized by the condensation of mechanochemically produced PBzMA macromonomer with a-methyl-w-aminopropoxy polyoxyethylene.
Although the polymeric micelles containing 5-fluorouracil (5-FU) or rohdamine showed the narrow size distribution as well as blank polymeric micelles, the particle diameter of the polymeric micelles containing 5-FU or rohdamine was larger than that of blank polymeric micelle.
Polymeric micelle containing 5-FU slowly released 5-FU and about 10 % of 5-FU was released within 72 h.
The present polymeric micelle was uptaken by A549 cells, but HepG2 cells did not.
Cytotoxicity of Polymeric micelle containing 5-FU was not observed against HepG2 and A549 cells in this experimental condition.
It was considered that the slow release of 5-FU from Polymeric micelle might cause the insufficient cytotoxicity.

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