Targeted delivery of 5-fluorouracil to HT-29 cells using high efficient folic acid-conjugated nanoparticles.

Wang,Y, Li,P, Chen,L, Gao,W, Zeng,F and Kong,LX 2015, Targeted delivery of 5-fluorouracil to HT-29 cells using high efficient folic acid-conjugated nanoparticles., Drug Delivery, vol. 22, no. 2, pp. 191-198, doi: 10.3109/10717544.2013.875603.

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Title Targeted delivery of 5-fluorouracil to HT-29 cells using high efficient folic acid-conjugated nanoparticles.
Author(s) Wang,Y
Gao,WORCID iD for Gao,W
Kong,LXORCID iD for Kong,LX
Journal name Drug Delivery
Volume number 22
Issue number 2
Start page 191
End page 198
Publisher Informa Healthcare
Place of publication England
Publication date 2015-02
ISSN 1521-0464
Keyword(s) HT-29
PLGA-1, 3-diaminopropane-folic acid
3-diaminopropane-folic acid
Summary Abstract The incorporation of a high percentage of targeting molecules into drug delivery system is one of the important methods for improving efficacy of targeting therapeutic drugs to cancer cells. PLGA-based drug delivery carriers with folic acid (FA) as targeting molecule have a low targeting efficiency due to a low FA conjugation ratio. In this work, we fabricated a FA-conjugated PLGA system using a crosslinker 1, 3-diaminopropane and have achieved a high conjugation ratio of 46.7% (mol/mol). The as-prepared PLGA-based biomaterial was used to encapsulate therapeutic drug 5-fluorouracil (5-FU) into nanoparticles. In the in vitro experiments, an IC50 of 5.69 µg/mL has been achieved for 5-FU loaded PLGA-1, 3-diaminopropane-folic acid nanoparticles on HT-29 cancer cells and is significantly lower than that of 5-FU and 5-FU loaded PLGA nanoparticles which only have an IC50 of 22.9 and 14.17 µg/mL, respectively. The fluorescent microscopy images showed that nanoparticles with FA are largely taken up by HT-29 cancer cells and the targeting nanoparticles have more affinity to cancer cells than the pure drugs and untreated nanoparticles. Therefore, the 1, 3-diaminopropane can facilitate the conjugation of FA to PLGA to form a novel polymer and 5-FU loaded PLGA-1, 3-diaminopropane-folic acid nanoparticles can be a highly efficient system for specific delivery of drugs to cancer cells.
Language eng
DOI 10.3109/10717544.2013.875603
Field of Research 030405 Molecular Medicine
Socio Economic Objective 920102 Cancer and Related Disorders
HERDC Research category C1 Refereed article in a scholarly journal
ERA Research output type C Journal article
Copyright notice ©2015, Informa Healthcare
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Document type: Journal Article
Collection: Institute for Frontier Materials
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