Conjugates of amphotericin B to resolve challenges associated with its delivery.

INTRODUCTION: Amphotericin B (AmB), a promising antifungal and antileishmanial drug, acts on the membrane of microorganisms. The clinical use of AmB is limited due to issues associated with its delivery including poor solubility and bioavailability, instability in acidic media, poor intestinal permeability, dose and aggregation state dependent toxicity, parenteral administration, and requirement of cold chain for transport and storage etc.

AREAS COVERED: Scientists have formulated and explored various covalent conjugates of AmB to reduce its toxicity with increase in solubility, oral bioavailability, and payload or loading of AmB by using various polymers, lipids, carbon based nanocarriers, metallic nanoparticles, and vesicular carriers etc. In this article, we have reviewed various conjugates of AmB with polymers and nanomaterials explored for its delivery to give a deep insight regarding further exploration in future.

EXPERT OPINION: Covalent conjugates of AmB have been investigated by scientists, and preliminary in vitro and animal investigations have given successful results, which are required to be validated further with systematic investigation on safety and therapeutic efficacy in animals followed by clinical trials.