An investigation of antitumor efficiency of novel sustained and targeted 5-fluorouracil nanoparticles

Le, VM; Wang, JJ; Yuan, M; Nguyen, TL; Yin, GF; Zheng, YH; Shi, WB; Lang, MD; Xu, LM; Liu, JW

An investigation of antitumor efficiency of novel sustained and targeted 5-fluorouracil nanoparticles

Le, VM Wang, JJ Yuan, M Nguyen, TL

Yin, GF Zheng, YH Shi, WB Lang, MD Xu, LM Liu, JW

Permalink

Publication Type:: Journal Article
Citation:: European Journal of Medicinal Chemistry, 2015, 92 pp. 882 - 889
Issue Date:: 2015-03-06

Closed Access

	Filename	Description	Size
	\\utsfs.adsroot.uts.edu.au\homes\staff\108848\Desktop\1-s2.0-S0223523414011520-main.pdf	Published Version	2.81 MB	Adobe PDF	View/Open

Copyright Clearance Process

Recently Added
In Progress
Closed Access

This item is closed access and not available.

Full metadata record

Field	Value	Language
dc.contributor.author	Le, VM	en_US
dc.contributor.author	Wang, JJ	en_US
dc.contributor.author	Yuan, M	en_US
dc.contributor.author	Nguyen, TL https://orcid.org/0000-0002-0630-4959	en_US
dc.contributor.author	Yin, GF	en_US
dc.contributor.author	Zheng, YH	en_US
dc.contributor.author	Shi, WB	en_US
dc.contributor.author	Lang, MD	en_US
dc.contributor.author	Xu, LM	en_US
dc.contributor.author	Liu, JW	en_US
dc.date.available	2014-12-24	en_US
dc.date.issued	2015-03-06	en_US
dc.identifier.citation	European Journal of Medicinal Chemistry, 2015, 92 pp. 882 - 889	en_US
dc.identifier.issn	0223-5234	en_US
dc.identifier.uri	http://hdl.handle.net/10453/118913
dc.description.abstract	© 2015 Published by Elsevier Masson SAS. Traditional chemotherapeutic drugs remain the major treatment for advanced colorectal cancer. However, due to the lack of tumor specificity these drug also destroy healthy tissue and organs, which has been the main reason for treatment failure and mortality. Folate-based drug delivery systems for improving nanoparticle endocytosis have been used to address these problems. Here, folic acid (FA) conjugated mPEG-b-P(CABCL-co-ACL) diblock copolymers were synthesized and characterized by TEM and NMR. Drug loaded nanoparticles were prepared using dialysis method and was obtained with a mean diameter of 45.2 nm with sustained in vitro release profile. In vitro cytotoxicity assay indicated that the cytotoxicity of folate modified nanoparticles were significantly increased compared to free drug and non-folate nanoparticles. In addition, results of hemolytic and histopathologic study suggested that the non-loaded nanoparticle (NL/NP) was non-toxic and biocompatible at the testing concentration. Moreover, in vivo results showed that FA/5-FU/NP effectively inhibited growth of HCT-8 cell-based xenograft tumors in BALB/c mice and revealed stronger antitumor efficacy than other treated groups. Thus, both in vitro and in vivo results exhibited that the folate conjugated mPEG-b-P(CABCL-co-ACL) copolymers have great potential to be used as sustainable and specific colon cancer targeting delivery system for anticancer agents.	en_US
dc.relation.ispartof	European Journal of Medicinal Chemistry	en_US
dc.relation.isbasedon	10.1016/j.ejmech.2014.12.043	en_US
dc.subject.classification	Medicinal & Biomolecular Chemistry	en_US
dc.subject.mesh	Cell Line, Tumor	en_US
dc.subject.mesh	HCT116 Cells	en_US
dc.subject.mesh	Animals	en_US
dc.subject.mesh	Mice, Inbred BALB C	en_US
dc.subject.mesh	Humans	en_US
dc.subject.mesh	Mice	en_US
dc.subject.mesh	Mice, Nude	en_US
dc.subject.mesh	Neoplasms, Experimental	en_US
dc.subject.mesh	Fluorouracil	en_US
dc.subject.mesh	Folic Acid	en_US
dc.subject.mesh	Polymers	en_US
dc.subject.mesh	Antineoplastic Agents	en_US
dc.subject.mesh	Drug Screening Assays, Antitumor	en_US
dc.subject.mesh	Apoptosis	en_US
dc.subject.mesh	Cell Proliferation	en_US
dc.subject.mesh	Structure-Activity Relationship	en_US
dc.subject.mesh	Dose-Response Relationship, Drug	en_US
dc.subject.mesh	Nanoparticles	en_US
dc.title	An investigation of antitumor efficiency of novel sustained and targeted 5-fluorouracil nanoparticles	en_US
dc.type	Journal Article
utslib.citation.volume	92	en_US
utslib.for	1115 Pharmacology and Pharmaceutical Sciences	en_US
utslib.for	0304 Medicinal and Biomolecular Chemistry	en_US
utslib.for	0305 Organic Chemistry	en_US
pubs.embargo.period	Not known	en_US
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Faculty of Science
utslib.copyright.status	closed_access
pubs.publication-status	Published	en_US
pubs.volume	92	en_US

Abstract:

© 2015 Published by Elsevier Masson SAS. Traditional chemotherapeutic drugs remain the major treatment for advanced colorectal cancer. However, due to the lack of tumor specificity these drug also destroy healthy tissue and organs, which has been the main reason for treatment failure and mortality. Folate-based drug delivery systems for improving nanoparticle endocytosis have been used to address these problems. Here, folic acid (FA) conjugated mPEG-b-P(CABCL-co-ACL) diblock copolymers were synthesized and characterized by TEM and NMR. Drug loaded nanoparticles were prepared using dialysis method and was obtained with a mean diameter of 45.2 nm with sustained in vitro release profile. In vitro cytotoxicity assay indicated that the cytotoxicity of folate modified nanoparticles were significantly increased compared to free drug and non-folate nanoparticles. In addition, results of hemolytic and histopathologic study suggested that the non-loaded nanoparticle (NL/NP) was non-toxic and biocompatible at the testing concentration. Moreover, in vivo results showed that FA/5-FU/NP effectively inhibited growth of HCT-8 cell-based xenograft tumors in BALB/c mice and revealed stronger antitumor efficacy than other treated groups. Thus, both in vitro and in vivo results exhibited that the folate conjugated mPEG-b-P(CABCL-co-ACL) copolymers have great potential to be used as sustainable and specific colon cancer targeting delivery system for anticancer agents.

Please use this identifier to cite or link to this item:

http://hdl.handle.net/10453/118913