Table of Contents
Pharmaceutics, Volume 10, Issue 4 (December 2018)
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Cover Story (view full-size image) The oral administration of clofazimine (CFZ), a WHO-recommended treatment for leprosy and [...] Read more. The oral administration of clofazimine (CFZ), a WHO-recommended treatment for leprosy and multi-drug resistant tuberculosis, has a major side effect: skin hyperpigmentation. Since CFZ is a weakly basic, red phenazine dye, the skin pigmentation results from the lipophilic partitioning of the circulating, free base (neutral) form of CFZ in the skin. Thus, we developed a stable and biocompatible formulation of CFZ–HCl microcrystals that mimics the predominant form of the CFZ that bioaccumulates in macrophages, following long-term oral CFZ administration. This formulation proved suitable for parenteral administration and could be instrumental to avoid the pigmentation side effect of oral CFZ therapy. View this paper.