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Super aggregated form of Amphotericin B: a novel way to increase its therapeutic index

Qamar Zia, Asim Azhar, Mohammad Amjad Kamal

  • 1Department of Biotechnology, Gagan College of Management and Technology, Aligarh, India Aligarh, India. gashraf@kau.edu.sa.

Current Pharmaceutical Design
|December 10, 2015
PubMed

Insights

A novel Amphotericin B (AmB) super-aggregate formulation shows reduced toxicity and maintains antifungal efficacy. This development offers a less toxic, more affordable alternative for treating serious fungal infections.

Area of Science:

  • Pharmacology
  • Mycology
  • Biochemistry

Background:

  • Fungizone®, the standard Amphotericin B (AmB) formulation, presents challenges due to long treatment durations and severe side effects.
  • Lipid-based AmB formulations are less toxic but expensive and may have reduced activity.
  • There is a need for a cost-effective and less toxic Amphotericin B alternative.

Purpose of the Study:

  • To develop and characterize a novel Amphotericin B (AmB) super-aggregate.
  • To evaluate the toxicity, efficacy, and biodistribution of the AmB super-aggregate compared to existing formulations.

Main Methods:

  • Spectroscopic analysis to distinguish AmB super-aggregate from Fungizone aggregate.
  • In vitro and in vivo toxicity studies in mammalian cells and mice.
  • Antifungal activity assays.
  • Serum albumin interaction studies.
  • Biodistribution studies focusing on kidney and reticulo-endothelial organs.

Main Results:

  • AmB super-aggregate is spectroscopically distinct and thermodynamically more stable than Fungizone aggregate.
  • Poly-aggregated AmB demonstrated reduced toxicity in vitro and in vivo.
  • The AmB super-aggregate maintained potent antifungal activity against target pathogens.
  • AmB super-aggregate preferentially binds to serum albumin, reducing cytokine induction.
  • Biodistribution studies showed increased accumulation in reticulo-endothelial organs and reduced kidney accumulation.

Conclusions:

  • AmB super-aggregate represents a promising alternative to existing Amphotericin B formulations.
  • This formulation offers improved therapeutic index by reducing toxicity while preserving antifungal efficacy.
  • The reduced toxicity and maintained activity make AmB super-aggregate suitable for treating various fungal infections like candidiasis and cryptococcosis.

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