Dendrimer-encapsulated camptothecins: Increased solubility, cellular uptake, and cellular retention affords enhanced anticancer activity in vitro.
- UNCG Author/Contributor (non-UNCG co-authors, if there are any, appear on document)
- Nicholas Oberlies, Patricia A. Sullivan Distinguished Professor of Chemistry (Creator)
- Institution
- The University of North Carolina at Greensboro (UNCG )
- Web Site: http://library.uncg.edu/
Abstract: A biocompatible polyester dendrimer composed of the natural metabolites, glycerol and succinic acid, is described for the encapsulation of the antitumor camptothecins, 10-hydroxycamptothecin and 7-butyl-10-aminocamptothecin. The cytotoxicity 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.
Dendrimer-encapsulated camptothecins: Increased solubility, cellular uptake, and cellular retention affords enhanced anticancer activity in vitro.
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Created on 1/1/2006
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Additional Information
- Publication
- Cancer Research. 66, 11913-11921.
- Language: English
- Date: 2006
- Keywords
- Biocompatible polyester dendrimer, Camptothecins