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Issue 15, 2012
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Synthesis of PEGylated fullerene–5-fluorouracil conjugates to enhance the antitumor effect of 5-fluorouracil

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Abstract

Many drugs have been delivered by different types of nanoscale vehicles to enhance their therapeutic efficacy. 5-Fluorouracil (5FU) is a widely used antitumor drug, however its bioavailability still needs to be improved. Herein we synthesized a polyethylene glycol monomethylether-C60–5FU conjugate (mPEG-C60–5FU) and evaluated its antitumor efficacy in vitro. The results show that the inhibition abilities of mPEG-C60–5FU to the human breast cancer cell line MCF-7 and the human gastric carcinoma cell line BGC-823 are significantly higher than that of 5FU. The conjugate has good stability in murine serum for at least 24 h. Moreover, the PEGylated fullerene (mPEG-C60) vehicle is non-toxic to MCF-7 cells. These results demonstrate that mPEG-C60 is an efficient vehicle for the delivery of 5FU.

Graphical abstract: Synthesis of PEGylated fullerene–5-fluorouracil conjugates to enhance the antitumor effect of 5-fluorouracil

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Article information


Submitted
17 Feb 2012
Accepted
21 May 2012
First published
25 May 2012

Nanoscale, 2012,4, 4624-4630
Article type
Paper

Synthesis of PEGylated fullerene–5-fluorouracil conjugates to enhance the antitumor effect of 5-fluorouracil

Z. Dou, Y. Xu, H. Sun and Y. Liu, Nanoscale, 2012, 4, 4624
DOI: 10.1039/C2NR30380A

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