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Amphotericin B formulations and drug targeting

J J Torrado1, R Espada, M P Ballesteros

  • 1Dpto Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Complutense University of Madrid, Plaza Ramón y Cajal, 28040 Madrid, Spain. torrado1@farm.ucm.es

Journal of Pharmaceutical Sciences
|September 26, 2007
PubMed

Insights

New Amphotericin B formulations improve treatment of fungal infections by altering drug delivery. These advanced formulations enhance efficacy and reduce toxicity, offering better patient outcomes.

Area of Science:

  • Pharmacology
  • Drug Delivery Systems
  • Antimicrobial Therapy

Background:

  • Amphotericin B (AMB) is a vital antibiotic for systemic fungal infections, despite its toxicity.
  • AMB's solubility and aggregation state significantly influence its pharmacokinetic profile and therapeutic activity.
  • Existing AMB formulations present challenges due to toxicity and variable efficacy.

Purpose of the Study:

  • To compare the pharmacokinetics, toxicity, and activity of various Amphotericin B formulations.
  • To evaluate the drug targeting potential of novel AMB delivery systems.
  • To review recent advancements in AMB formulations for improved therapeutic ratios.

Main Methods:

  • Comparative analysis of published data on Amphotericin B formulations.
  • Review of pharmacokinetic studies for different AMB delivery systems (liposomes, nanospheres, microspheres).
  • Assessment of clinical efficacy and toxicity profiles of marketed AMB formulations.

Main Results:

  • Novel formulations (liposomal, nanospheres, microspheres) alter AMB distribution, increasing liver/spleen concentrations and decreasing kidney/lung concentrations.
  • These advanced drug delivery systems can reduce AMB toxicity while potentially enhancing drug accessibility to specific tissues like bone marrow.
  • Newer AMB formulations like AmBisome, Abelcet, and Amphotec demonstrate an improved efficacy/toxicity ratio.

Conclusions:

  • Formulation significantly impacts Amphotericin B's pharmacokinetic and toxicological properties.
  • Advanced drug delivery systems offer promising strategies for targeted delivery and reduced toxicity of Amphotericin B.
  • Recent Amphotericin B formulations provide enhanced therapeutic options for systemic fungal infections.

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