Issue 79, 2012

Enhanced stability and activity of temozolomide in primary glioblastoma multiforme cells with cucurbit[n]uril

Abstract

Temozolomide (TMZ) is the primary chemotherapeutic agent for treatment of glioblastoma multiforme (GBM) yet it has a fast rate of degradation under physiological conditions to the ‘active’ MTIC, which has poor penetration of the blood–brain barrier and cellular absorption. Herein we have demonstrated binding of TMZ within the cavity of nano-container cucurbit[7]uril, resulting in a decreased rate of drug degradation. Prolonging the lifetime of the TMZ under physiological conditions through encapsulation dramatically improved the drug's activity against primary GBM cell lines as more TMZ could be absorbed by the cells before degradation. This work can potentially lead to increases in the drug's propensity for crossing the blood–brain barrier and absorption into the GBM cells, thereby increasing the efficacy of this chemotherapy.

Graphical abstract: Enhanced stability and activity of temozolomide in primary glioblastoma multiforme cells with cucurbit[n]uril

Supplementary files

Article information

Article type
Communication
Submitted
17 Jul 2012
Accepted
15 Aug 2012
First published
30 Aug 2012

Chem. Commun., 2012,48, 9843-9845

Enhanced stability and activity of temozolomide in primary glioblastoma multiforme cells with cucurbit[n]uril

E. A. Appel, M. J. Rowland, X. J. Loh, R. M. Heywood, C. Watts and O. A. Scherman, Chem. Commun., 2012, 48, 9843 DOI: 10.1039/C2CC35131E

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