Review of Novel Oral Amphotericin B Formulations for the Treatment of Parasitic Infections

Pharmaceutics. 2022 Oct 28;14(11):2316. doi: 10.3390/pharmaceutics14112316.

Abstract

Amphotericin B (AmpB) is a polyene macrolide antibiotic used in the treatment of blood-borne parasitic and fungal infections. However, its use, particularly in the developing world, has been limited by dose-dependent kidney toxicity, other systemic-related toxicity issues following injection, the inconvenience of parenteral administration, and accessibility. Oral formulation approaches have focused on the dual problem of solubility and permeability of AmpB, which is poorly water soluble, amphoteric and has extremely low oral bioavailability. Therefore, to enhance oral absorption, researchers have employed micellar formulations, polymeric nanoparticles, cochleates, pro-drugs, and self-emulsifying drug delivery systems (SEDDS). This paper will highlight current uses of AmpB against parasitic infections such as leishmaniasis, preclinical and clinical formulation strategies, applications in veterinary medicine and the importance of developing a cost-effective and safe oral AmpB formulation.

Keywords: SEDDS; drug delivery; human use; nanomedicines; nanoparticles; oral amphotericin B; parasitic infections; pharmacokinetics; safety and tolerability; veterinary use.

Publication types

  • Review

Grants and funding

This oral amphotericin B formulation studies project were funded by the Canadian Institutes of Health Research to KMW and EKW, Consortium of Parasitic Drug Develop 394 (Gates Foundation Grantee) and iCo Therapeutics Inc. (Currently Satellos Biosciences Inc.).