Dendrimer-encapsulated camptothecins:: Increased solubility, cellular uptake, and cellular retention affords enhanced anticancer activity in vitro

被引：224

作者：

Morgan, Meredith T.

Nakanishi, Yuka

Kroll, David J. ^{[1
]}

Griset, Aaron P.

Carnahan, Michael A.

Wathier, Michel

Oberlies, Nicholas H.

Manikumar, Govindarajan

Wani, Mansukh C.

Grinstaff, Mark W.

机构：

[1] Res Triangle Inst, Nat Prod Lab, Res Triangle Pk, NC 27709 USA

[2] Duke Univ, Dept Chem, Durham, NC 27706 USA

[3] Duke Univ, Med Ctr, Dept Ophthalmol, Durham, NC 27710 USA

[4] Boston Univ, Dept Biomed Engn, Boston, MA 02215 USA

[5] Boston Univ, Metcalf Ctr Sci & Engn, Dept Chem, Boston, MA 02215 USA

来源：

CANCER RESEARCH | 2006年 / 66卷 / 24期

关键词：

DRUG-DELIVERY; BIOMEDICAL APPLICATIONS; CURRENT PERSPECTIVES; PAMAM DENDRIMERS; NATURAL-PRODUCTS; RELEASE; PHARMACOLOGY; IRINOTECAN; ADHESIVES; TOXICITY;

D O I：

10.1158/0008-5472.CAN-06-2066

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

A biocompatible polyester dendrimer composed of the natural metabolites, glycerol and succinic acid, is described for the encapsulation of the antitumor camptothecins, 10-hydroxy-camptothecin and 7-butyl-10-aminocamptothecin. The cyto-toxicity of the dendrimer-drug complex toward four different human cancer cell lines [human breast adenocarcinoma (MCF-7). colorectal adenocarcinoma (HT-29), non-small cell lung carcinoma (NCI-H460), and glioblastoma (SF-268)] is also reported, and low nmol/L IC50 values are measured. Cellular uptake and efflux measurements in MCF-7 cells show an increase of 16-fold for cellular uptake and an increase in drug retention within the cell when using the dendrimer vehicle.

引用

页码：11913 / 11921

页数：9

共 51 条

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