Additive potential of combination therapy against cryptococcosis employing a novel amphotericin B and fluconazole loaded dual delivery system

Eur J Pharm Sci. 2018 Jul 1:119:171-178. doi: 10.1016/j.ejps.2018.04.015. Epub 2018 Apr 11.

Abstract

Cryptococcus neoformans is one of the most lethal fungi causing mortality across the globe. Immuno-competent patients and patients taking immuno-suppressive medications are extremely susceptible to its infection. For effective removal of cryptococcal burden, there is an urgent need for new forms of therapy. In the present study, we have explored the potential effects of amphotericin B (AMB) and fluconazole (FLC) in combination, against cryptococcosis in Swiss albino mice. To enhance the therapeutic potential of the tested drugs, they were entrapped into fibrin microspheres; a dual delivery vehicle comprising of poly-lactide co-glycolide (PLGA) microsphere that was additionally encapsulated into the fibrin cross-linked plasma bead. Dynamics of fibrin microspheres included survival and fungal burden in lung, liver and spleen of treated mice. While each drug was effective in combination or alone, prominent additive potential of AMB and FLC were clearly observed when used in fibrin microsphere. Significant reduction in fungal burden and increase in survival rate of AMB + FLC-fibrin microspheres treated mice shows an extensive accessibility of both tested drugs without any side-effects. A full potential of two-drug combination encapsulated in fibrin microspheres proposes an effective approach of safe delivery to the target site in their intact form and decrease the drug associated toxicities.

Keywords: Combination therapy; Cryptococcus neoformans; Dual delivery; Fibrin microspheres; PLGA microspheres.

MeSH terms

  • Amphotericin B / administration & dosage*
  • Amphotericin B / chemistry
  • Amphotericin B / therapeutic use
  • Animals
  • Antifungal Agents / administration & dosage*
  • Antifungal Agents / chemistry
  • Antifungal Agents / therapeutic use
  • Cryptococcosis / drug therapy*
  • Cryptococcus neoformans / drug effects
  • Cryptococcus neoformans / growth & development
  • Drug Combinations
  • Drug Delivery Systems
  • Drug Liberation
  • Drug Synergism
  • Fluconazole / administration & dosage*
  • Fluconazole / chemistry
  • Fluconazole / therapeutic use
  • Lactic Acid / administration & dosage
  • Lactic Acid / chemistry
  • Male
  • Mice
  • Microbial Sensitivity Tests
  • Microspheres
  • Polyglycolic Acid / administration & dosage
  • Polyglycolic Acid / chemistry
  • Polylactic Acid-Polyglycolic Acid Copolymer

Substances

  • Antifungal Agents
  • Drug Combinations
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Amphotericin B
  • Fluconazole