Effect of Liposome and Cyclodextrin Entrapment on Retardation of Glutathione Decomposition of Nitroimidazolyl Sulfones

摘要: A new class of radiosensitizing pharmaceuticals derived from 4-nitro-5-imidazolyl sulfones has its clinical potential compromised by a metabolic reaction with plasma glutathione which leads to much less active metabolite. Entrapment two members the in three different liposomes, one polymerized liposome, and β-cyclodextrin system shown that this condensation can be suppressed rate factor nearly 50-fold. Stabilizations these metabolically labile radiosensitizers appear relate their lipid−buffer partition coefficients fluidity liposome membrane they are entrapped.