Effect of liposome and cyclodextrin entrapment on retardation of glutathione decomposition of nitroimidazolyl sulfones

Ned D. Heindel, Roger A. Egolf, James S. Stefely

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

Abstract

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 a much less active metabolite. Entrapment of two members of the class in three different liposomes, one polymerized liposome, and a β‐cyclodextrin system has shown that this glutathione condensation can be suppressed by a rate factor of nearly 50‐fold. Stabilizations of these metabolically labile radiosensitizers appear to relate to their lipid‐buffer partition coefficients and to the fluidity of the liposome membrane in which they are entrapped.

Original languageEnglish (US)
Pages (from-to)862-865
Number of pages4
JournalJournal of Pharmaceutical Sciences
Volume79
Issue number10
DOIs
StatePublished - Oct 1990

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Fingerprint Dive into the research topics of 'Effect of liposome and cyclodextrin entrapment on retardation of glutathione decomposition of nitroimidazolyl sulfones'. Together they form a unique fingerprint.

Cite this