期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 44, 期 2, 页码 862-868出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2008.04.021
关键词
Dendrimer; Cancer targeting; Biotin; Conjugate; Nano-carrier
资金
- Ministry of Science and Technology of China [2006CB933300]
- Natural Science Foundation of Anhui Province [070413112]
- Innovation Foundation from Hefei National Laboratory for Physical Sciences at Microscale [C07-06]
Star-burst dendrimers represent a superior carrier platform for targeted drug delivery. Partially acetylated generation 5 (G5) polyamidoamine (PAMAM) dendrimer was conjugated with the targeting moiety (biotin) and the imaging moiety (fluoresceinisothiocyanate, FITC), and the resulting dendrimer-biotin conjugate was characterized by H-1 NMR, UV-vis spectrum. As revealed by flow cytometry and confocal microscopy, the bifunctional conjugate (dendrimer-biotin-FITC) exhibited much higher cellular uptake into HeLa cells than the conjugate without biotin. The uptake was energy-dependent, dose-dependent, and could be effectively blocked by dendrimer-conjugated biotin. Our results indicated that the biocompatible biotin-dendrimer conjugate might be a promising nano-platform for cancer therapy and cancer diagnosis. (c) 2008 Elsevier Masson SAS. All rights reserved.
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