Pharmacodynamics of folic acid receptor targeted antiretroviral nanotherapy in HIV-1-infected humanized mice

Antiviral Res. 2015 Aug:120:85-8. doi: 10.1016/j.antiviral.2015.05.009. Epub 2015 May 27.

Abstract

Long-acting nanoformulated antiretroviral therapy (nanoART) can sustain plasma drug levels and improve its biodistribution. Cell targeted-nanoART can achieve this and bring drug efficiently to viral reservoirs. However, whether such improvements affect antiretroviral responses remains unknown. To these ends, we tested folic acid (FA)-linked poloxamer407-coated ritonavir-boosted atazanavir (FA-nanoATV/r) nanoparticles for their ability to affect chronic HIV-1 infection in humanized mice. Following three, 100mg/kg FA-nanoATV/r intramuscular injections administered every other week to infected animals, viral RNA was at or below the detection limit, cell-associated HIV-1p24 reduced and CD4+ T cell counts protected. The dosing regimen improved treatment outcomes more than two fold from untargeted nanoATV/r. We posit that these nanoformulations have potential for translation to human use.

Keywords: Folic acid receptor; Human immunodeficiency virus type one; Long-acting nanoformulated antiretroviral therapy; Non-obese diabetic severe combined immunodeficient mice; Pharmacodynamics; Pharmacokinetics.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Retroviral Agents / administration & dosage
  • Anti-Retroviral Agents / pharmacokinetics*
  • Atazanavir Sulfate / administration & dosage
  • Atazanavir Sulfate / pharmacokinetics
  • CD4 Lymphocyte Count
  • Delayed-Action Preparations / administration & dosage
  • Delayed-Action Preparations / pharmacokinetics*
  • Drug Carriers / administration & dosage
  • Drug Carriers / metabolism*
  • Folate Receptors, GPI-Anchored / metabolism*
  • Folic Acid / administration & dosage
  • Folic Acid / metabolism
  • HIV Infections / drug therapy
  • Humans
  • Injections, Intramuscular
  • Mice, SCID
  • Nanomedicine / methods*
  • Nanoparticles / administration & dosage
  • Nanoparticles / metabolism*
  • Poloxamer / administration & dosage
  • Poloxamer / metabolism
  • RNA, Viral / blood
  • Ritonavir / administration & dosage
  • Ritonavir / pharmacokinetics
  • Treatment Outcome
  • Viral Load

Substances

  • Anti-Retroviral Agents
  • Delayed-Action Preparations
  • Drug Carriers
  • Folate Receptors, GPI-Anchored
  • RNA, Viral
  • Poloxamer
  • Atazanavir Sulfate
  • Folic Acid
  • Ritonavir