UM  > 中華醫藥研究院
PH-sensitive micelles based on acid-labile pluronic F68-curcumin conjugates for improved tumor intracellular drug delivery
Fang X.-B.1; Zhang J.-M.1; Xie X.2; Liu D.3; He C.-W.1; Wan J.-B.1; Chen M.-W.1
2016
Source PublicationInternational Journal of Pharmaceutics
ISSN3785173
Volume502Issue:2018-01-02Pages:28
Abstract

Curcumin (Cur) is a highly pleiotropic anticancer agent that inhibits cell proliferation and induces apoptosis in cancer cells. A variety of nano-systems constituted by polymer-drug conjugates have been designed to overcome its shortages on water solubility, chemical instability, and poor bioavailability. However, most of them suffer from ineffective release of Cur in cancer cells in vivo. This work developed a novel flexible acid-responsive micelle formulation by covalently conjugating Cur on the hydrophilic terminals of pluronic F68 chains via cis-aconitic anhydride linkers. The synthesized F68-Cis-Cur conjugates can readily precipitate to form homogeneous micelles with average size about 100 nm in aqueous solution. In acid environments, F68-Cis-Cur conjugates would break down and subsequently release Cur rapidly, for the reason of pH-sensitive cleavage of cis-aconitic anhydride linkers. In vitro anticancer activity tests demonstrated that F68-Cis-Cur micelles induced higher cytotoxicity against both A2780 and SMMC 7721 cells than free Cur. It provided a larger decrease of mitochondrion membrane potential and induced cellular apoptosis. F68-Cis-Cur micelles remarkably increased cellular uptake of Cur than free Cur through caveolae-mediated endocytosis in an energy-dependent manner. This study demonstrates F68-Cis-Cur conjugation as a promising tool for improving intracellular drug delivery in cancer therapy.

KeywordCancer Curcumin Ph-sensitive Pluronic F68 Polymer-drug Conjugate
DOI10.1016/j.ijpharm.2016.01.029
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000372814700004
The Source to ArticleScopus
Fulltext Access
Citation statistics
Cited Times [WOS]:34   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorChen M.-W.
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Taipa, Macau 999078, China
2.School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou 510275, China
3.School of Mathematics, University of Minnesota, Minneapolis, MN 55455, USA
First Author AffilicationInstitute of Chinese Medical Sciences
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Fang X.-B.,Zhang J.-M.,Xie X.,et al. PH-sensitive micelles based on acid-labile pluronic F68-curcumin conjugates for improved tumor intracellular drug delivery[J]. International Journal of Pharmaceutics,2016,502(2018-01-02):28.
APA Fang X.-B..,Zhang J.-M..,Xie X..,Liu D..,He C.-W..,...&Chen M.-W..(2016).PH-sensitive micelles based on acid-labile pluronic F68-curcumin conjugates for improved tumor intracellular drug delivery.International Journal of Pharmaceutics,502(2018-01-02),28.
MLA Fang X.-B.,et al."PH-sensitive micelles based on acid-labile pluronic F68-curcumin conjugates for improved tumor intracellular drug delivery".International Journal of Pharmaceutics 502.2018-01-02(2016):28.
Related Services
Recommend this item
Bookmark
Usage statistics
Export to Endnote
Google Scholar
Similar articles in Google Scholar
[Fang X.-B.]'s Articles
[Zhang J.-M.]'s Articles
[Xie X.]'s Articles
Baidu academic
Similar articles in Baidu academic
[Fang X.-B.]'s Articles
[Zhang J.-M.]'s Articles
[Xie X.]'s Articles
Bing Scholar
Similar articles in Bing Scholar
[Fang X.-B.]'s Articles
[Zhang J.-M.]'s Articles
[Xie X.]'s Articles
Terms of Use
No data!
Social Bookmark/Share
All comments (0)
No comment.
 

Items in the repository are protected by copyright, with all rights reserved, unless otherwise indicated.