Improving aqueous solubility and antitumor effects by nanosized gambogic acid-mPEG2000 micelles

The clinical application of gambogic acid, a natural component with promising antitumor activity, is limited due to its extremely poor aqueous solubility, short half-life in blood, and severe systemic toxicity. To solve these problems, an amphiphilic polymer-drug conjugate was prepared by attachment...

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Main Authors:	Cai, Lulu, Qiu, Neng, Xiang, Mingli, Tong, Rongsheng, Yan, Junfeng, He, Lin, Shi, Jianyou, Chen, Tao, Wen, Jiaolin, Wang, Wenwen, Chen, Lijuan
Format:	Online
Language:	English
Published:	Dove Medical Press 2013
Online Access:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3883552/

id	pubmed-3883552
recordtype	oai_dc
spelling	pubmed-38835522014-01-08 Improving aqueous solubility and antitumor effects by nanosized gambogic acid-mPEG2000 micelles Cai, Lulu Qiu, Neng Xiang, Mingli Tong, Rongsheng Yan, Junfeng He, Lin Shi, Jianyou Chen, Tao Wen, Jiaolin Wang, Wenwen Chen, Lijuan Original Research The clinical application of gambogic acid, a natural component with promising antitumor activity, is limited due to its extremely poor aqueous solubility, short half-life in blood, and severe systemic toxicity. To solve these problems, an amphiphilic polymer-drug conjugate was prepared by attachment of low molecular weight (ie, 2 kDa) methoxy poly(ethylene glycol) methyl ether (mPEG) to gambogic acid (GA-mPEG2000) through an ester linkage and characterized by 1H nuclear magnetic resonance. The GA-mPEG2000 conjugates self-assembled to form nanosized micelles, with mean diameters of less than 50 nm, and a very narrow particle size distribution. The properties of the GA-mPEG2000 micelles, including morphology, stability, molecular modeling, and drug release profile, were evaluated. MTT (3-(4,5-dimethylthiazo l-2-yl)-2,5 diphenyl tetrazolium bromide) tests demonstrated that the GA-mPEG2000 micelle formulation had obvious cytotoxicity to tumor cells and human umbilical vein endothelial cells. Further, GA-mPEG2000 micelles were effective in inhibiting tumor growth and prolonged survival in subcutaneous B16-F10 and C26 tumor models. Our findings suggest that GA-mPEG2000 micelles may have promising applications in tumor therapy. Dove Medical Press 2013-12-27 /pmc/articles/PMC3883552/ /pubmed/24403830 http://dx.doi.org/10.2147/IJN.S54050 Text en © 2014 Cai et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.
repository_type	Open Access Journal
institution_category	Foreign Institution
institution	US National Center for Biotechnology Information
building	NCBI PubMed
collection	Online Access
language	English
format	Online
author	Cai, Lulu Qiu, Neng Xiang, Mingli Tong, Rongsheng Yan, Junfeng He, Lin Shi, Jianyou Chen, Tao Wen, Jiaolin Wang, Wenwen Chen, Lijuan
spellingShingle	Cai, Lulu Qiu, Neng Xiang, Mingli Tong, Rongsheng Yan, Junfeng He, Lin Shi, Jianyou Chen, Tao Wen, Jiaolin Wang, Wenwen Chen, Lijuan Improving aqueous solubility and antitumor effects by nanosized gambogic acid-mPEG2000 micelles
author_facet	Cai, Lulu Qiu, Neng Xiang, Mingli Tong, Rongsheng Yan, Junfeng He, Lin Shi, Jianyou Chen, Tao Wen, Jiaolin Wang, Wenwen Chen, Lijuan
author_sort	Cai, Lulu
title	Improving aqueous solubility and antitumor effects by nanosized gambogic acid-mPEG2000 micelles
title_short	Improving aqueous solubility and antitumor effects by nanosized gambogic acid-mPEG2000 micelles
title_full	Improving aqueous solubility and antitumor effects by nanosized gambogic acid-mPEG2000 micelles
title_fullStr	Improving aqueous solubility and antitumor effects by nanosized gambogic acid-mPEG2000 micelles
title_full_unstemmed	Improving aqueous solubility and antitumor effects by nanosized gambogic acid-mPEG2000 micelles
title_sort	improving aqueous solubility and antitumor effects by nanosized gambogic acid-mpeg2000 micelles
description	The clinical application of gambogic acid, a natural component with promising antitumor activity, is limited due to its extremely poor aqueous solubility, short half-life in blood, and severe systemic toxicity. To solve these problems, an amphiphilic polymer-drug conjugate was prepared by attachment of low molecular weight (ie, 2 kDa) methoxy poly(ethylene glycol) methyl ether (mPEG) to gambogic acid (GA-mPEG2000) through an ester linkage and characterized by 1H nuclear magnetic resonance. The GA-mPEG2000 conjugates self-assembled to form nanosized micelles, with mean diameters of less than 50 nm, and a very narrow particle size distribution. The properties of the GA-mPEG2000 micelles, including morphology, stability, molecular modeling, and drug release profile, were evaluated. MTT (3-(4,5-dimethylthiazo l-2-yl)-2,5 diphenyl tetrazolium bromide) tests demonstrated that the GA-mPEG2000 micelle formulation had obvious cytotoxicity to tumor cells and human umbilical vein endothelial cells. Further, GA-mPEG2000 micelles were effective in inhibiting tumor growth and prolonged survival in subcutaneous B16-F10 and C26 tumor models. Our findings suggest that GA-mPEG2000 micelles may have promising applications in tumor therapy.
publisher	Dove Medical Press
publishDate	2013
url	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3883552/
_version_	1612045086222188544

Improving aqueous solubility and antitumor effects by nanosized gambogic acid-mPEG2000 micelles

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