1. Background of Technology

Polyene Macrolides is the major class of drug for fungal infection, including amphotericin B (Ambisome, Astellas; Abelcet, Enzon; Fungizone, Apothecon), nystatin (Mycostatin, Westwood Squibb), griseofluvin (Fulvicin, Schering). 

Among these, amphotericin B is most commonly and conventionally used since 1960's. Amphotericin B is the mainstay antifungal agent for treatment of life-threatening mycoses and for most other mycoses, with the possible exception of the dermatophytoses. It binds to ergosterol to form ion channels and this disruption of membrane causes leakage of intracellular cations, causing cell death. Its broad spectrum of activity includes most of the medically important moulds and yeasts, including dimorphic pathogens such as Coccidioides immitis, Histoplasma capsulatum, Blastomyces dermatitidis, and Paracoccidioides brasiliensis. It is the drug of choice in treating most opportunistic mycoses caused by fungi such as Candida species, Cryptococcus neoformans, Aspergillus species, and the Zygomycetes.

Amphotericin B, however, must be administered intravenously and is associated with numerous side effects, ranging from phlebitis at the infusion site and chills to renal toxicity, which may be severe. Therefore, a new type of anti-fungal treatment needs to be actively sought which still has broad-spectrum antifungal activity with much-reduced side-effect, if any.

2. Description on Technology

Applied