UM  > 中華醫藥研究院
Nucleolin targeting AS1411 aptamer modified pH-sensitive micelles for enhanced delivery and antitumor efficacy of paclitaxel
Zhang J.1; Chen R.1; Fang X.2; Chen F.1; Wang Y.1; Chen M.1
2015
Source PublicationNano Research
ISSN19980124
Volume8Issue:1Pages:201
Abstract

Targeted drug delivery coupled with rapid drug release in cytoplasm is a powerful strategy to enhance efficacy and reduce off-target effects of anti-cancer drugs. Herein, we describe a dual-functional mixed micellar system consisting of a pH-responsive copolymer D-α-tocopheryl polyethylene glycol 1000-blockpoly-(β-amino ester) (TPGS-b-PBAE, TP) and AS1411 aptamer (Apt) decorated TPGS polymer (Apt-TPGS), which recognizes the over-expressed nucleolin on the plasma membrane of cancer cells. The anti-cancer drug paclitaxel (PTX) was encapsulated in the Apt-mixed micelles, and these drug-loaded micelles had a suitable particle size and zeta potential of 116.3 nm ± 12.4 nm and −26.2 mV ±4.2 mV, respectively. PTX/Apt-mixed micelles were stable at pH 7.4, but they dissociated and quickly released the encapsulated PTX in a weakly acidic environment (pH 5.5). Compared with non-Apt modified mixed micelles, more Apt-modified mixed micelles were internalized in SKOV3 ovarian cancer cells, whereas no significant difference in cellular uptake was observed in normal cells (LO2 cells). The enhanced transmembrane ability of Apt-modified mixed micelles was achieved through Apt-nucleolin interaction. With a synergistic effect of cancer cell recognition and pH-sensitive drug release, we observed significantly increased cytotoxicity and G2/M phase arrest against SKOV3 cells by PTX/Apt-mixed micelles. Intravenous administration of PTX/Apt-mixed micelles for 16 days significantly increased tumor accumulation of PTX, inhibited tumor growth, and reduced myelosuppression on tumor-bearing mice compared with free PTX injection. Therefore, this dual-functional Apt-mixed micellar system is a promising drug delivery system for targeted cancer therapy. © 2015, Tsinghua University Press and Springer-Verlag Berlin Heidelberg.

KeywordAs1411 Aptamer Micelles Ovarian Cancer Paclitaxel Ph-sensitive
DOIhttp://doi.org/10.1007/s12274-014-0619-4
URLView the original
Indexed BySCI
Language英语
WOS Research AreaChemistry ; Science & Technology - Other Topics ; Materials Science ; Physics
WOS SubjectChemistry, Physical ; Nanoscience & Nanotechnology ; Materials Science, Multidisciplinary ; Physics, Applied
WOS IDWOS:000348200300016
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 AuthorWang Y.; Chen M.
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical SciencesUniversity of MacauMacaoChina
2.Department of Pediatrics, College of MedicineUniversity of FloridaGainesvilleUSA
First Author AffilicationInstitute of Chinese Medical Sciences
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Zhang J.,Chen R.,Fang X.,et al. Nucleolin targeting AS1411 aptamer modified pH-sensitive micelles for enhanced delivery and antitumor efficacy of paclitaxel[J]. Nano Research,2015,8(1):201.
APA Zhang J.,Chen R.,Fang X.,Chen F.,Wang Y.,&Chen M..(2015).Nucleolin targeting AS1411 aptamer modified pH-sensitive micelles for enhanced delivery and antitumor efficacy of paclitaxel.Nano Research,8(1),201.
MLA Zhang J.,et al."Nucleolin targeting AS1411 aptamer modified pH-sensitive micelles for enhanced delivery and antitumor efficacy of paclitaxel".Nano Research 8.1(2015):201.
Related Services
Recommend this item
Bookmark
Usage statistics
Export to Endnote
Google Scholar
Similar articles in Google Scholar
[Zhang J.]'s Articles
[Chen R.]'s Articles
[Fang X.]'s Articles
Baidu academic
Similar articles in Baidu academic
[Zhang J.]'s Articles
[Chen R.]'s Articles
[Fang X.]'s Articles
Bing Scholar
Similar articles in Bing Scholar
[Zhang J.]'s Articles
[Chen R.]'s Articles
[Fang 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.