Review : Cremophor: Pharmacological activity of an "inert" solubiliser

Abstract

Objective. To provide an overview of the known pharmacological activity of the solvent for pacli taxel, Cremophor, and the implications for therapy with paclitaxel. Data Sources. Following an outline of the chemistry of Cremophor and its potential to cause hypersensitivity, we present a summary of our own results from studies on the effect of Cremophor as an MDR modulator. Data Extraction. The pharmacokinetic inter actions of paclitaxel and Cremophor are discussed, with reference to our own preclinical and clinical studies of Cremophor, and literature reports of altered drug disposition following combination therapy with paclitaxel are examined. Data Synthesis. Cremophor is not an inert solubiliser. Cremophor may contribute to drug interactions by altering drug disposition, and it has the ability to modulate multidrug resistance. As a consequence of the presence of Cremophor in the paclitaxel formulation, the use of paclitaxel should be considered as the administration of two agents.