期刊
CHEMICAL COMMUNICATIONS
卷 48, 期 79, 页码 9843-9845出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2cc35131e
关键词
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资金
- Schlumberger
- University of Cambridge Chemical Biology and Molecular Medicine program
- A*STAR
- Sims Scholarship at the University of Cambridge
- NIHR Cambridge Biomedical Research Centre
- ERC Starting Investigator Grant (ASPiRe)
- Walters-Kundert Foundation
- Engineering and Physical Sciences Research Council [EP/F035535/1] Funding Source: researchfish
- Medical Research Council [G108/507] Funding Source: researchfish
- EPSRC [EP/F035535/1] Funding Source: UKRI
- MRC [G108/507] Funding Source: UKRI
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.
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