Noncovalent complexation of amphotericin-B with Poly(α-glutamic acid)

Mol Pharm. 2013 Mar 4;10(3):940-50. doi: 10.1021/mp300339p. Epub 2013 Feb 8.

Abstract

A noncovalent complex of amphotericin B (AmB) and poly(α-glutamic acid) (PGA) was prepared to develop a safe and stable formulation for the treatment of leishmaniasis. The loading of AmB in the complex was in the range of ∼20-50%. AmB was in a highly aggregated state with an aggregation ratio often above 2.0. This complex (AmB-PGA) was shown to be stable and to have reduced toxicity to human red blood cells and KB cells compared to the parent compound; cell viability was not affected at an AmB concentration as high as 50 and 200 μg/mL respectively. This AmB-PGA complex retained AmB activity against intracellular Leishmania major amastigotes in the differentiated THP-1 cells with an EC50 of 0.07 ± 0.03-0.08 ± 0.01 μg/mL, which is similar to Fungizone (EC50 of 0.06 ± 0.01 μg/mL). The in vitro antileishmanial activity of the complex against Leishmania donovani was retained after storage at 37 °C for 7 days in the form of a solution (EC50 of 0.27 ± 0.03 to 0.35 ± 0.04 μg/mL) and for 30 days as a solid (EC50 of 0.41 ± 0.07 to 0.63 ± 0.25 μg/mL). These encouraging results indicate that the AmB-PGA complex has the potential for further development.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amphotericin B / chemistry*
  • Amphotericin B / pharmacology*
  • Amphotericin B / therapeutic use
  • Cell Line
  • Glutamic Acid / chemistry*
  • Humans
  • Leishmania donovani / drug effects
  • Leishmania major / drug effects
  • Leishmania major / pathogenicity
  • Leishmaniasis / drug therapy
  • Solubility

Substances

  • Glutamic Acid
  • Amphotericin B