• Journal Article

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

Citation

Morgan, M. T., Nakanishi, Y., Kroll, D., Griset, A. P., Carnahan, M. A., Wathier, M., ... Grinstaff, M. W. (2006). Dendrimer-encapsulated camptothecins: Increased solubility, cellular uptake, and cellular retention affords enhanced anticancer activity in vitro. Cancer Research, 66(24), 11913-11921. DOI: 10.1158/0008-5472.CAN-06-2066

Abstract

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