Antileishmanial activity, uptake, and biodistribution of an amphotericin B and poly(α-Glutamic Acid) complex

Antimicrob Agents Chemother. 2013 Oct;57(10):4608-14. doi: 10.1128/AAC.02343-12. Epub 2013 Jun 24.

Abstract

A noncovalent, water-soluble complex of amphotericin B (AMB) and poly(α-glutamic acid) (PGA), with AMB loadings ranging from 25 to 55% (wt/wt) using PGA with a molecular weight range of 50,000 to 70,000, was prepared as a potential new treatment for visceral leishmaniasis (VL). The AMB-PGA complex was shown to be as active as Fungizone (AMB deoxycholate) against intracellular Leishmania donovani amastigotes in differentiated THP-1 cells. The in vitro uptake of the AMB-PGA complex by differentiated THP-1 cells was similar to that of Fungizone and higher than that of AmBisome (liposomal AMB). The AMB-PGA complex also displayed a dose-response profile similar to that of AmBisome in vivo in BALB/c mice against L. donovani, with 50% effective doses (ED50s) of 0.24 ± 0.03 mg/kg of body weight for the AMB-PGA complex and 0.24 ± 0.06 mg/kg for AmBisome. A biodistribution study with mice indicated that the AMB-PGA complex cleared more rapidly from plasma than AmBisome, with a comparable low level of distribution to the kidneys.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amphotericin B / chemistry*
  • Amphotericin B / pharmacology*
  • Amphotericin B / therapeutic use
  • Animals
  • Antiprotozoal Agents / chemistry*
  • Antiprotozoal Agents / pharmacology*
  • Antiprotozoal Agents / therapeutic use
  • Cell Line
  • Drug Combinations
  • Female
  • Humans
  • Leishmania donovani / drug effects
  • Leishmania donovani / pathogenicity
  • Leishmaniasis, Visceral / drug therapy
  • Mice
  • Mice, Inbred BALB C
  • Polyglutamic Acid / chemistry*

Substances

  • Antiprotozoal Agents
  • Drug Combinations
  • liposomal amphotericin B
  • Polyglutamic Acid
  • Amphotericin B