Development of an extended action fostemsavir lipid nanoparticle

Commun Biol. 2024 Jul 30;7(1):917. doi: 10.1038/s42003-024-06589-5.

Abstract

An extended action fostemsavir (FTR) lipid nanoparticle (LNP) formulation prevents human immunodeficiency virus type one (HIV-1) infection. This FTR formulation establishes a drug depot in monocyte-derived macrophages that extend the drug's plasma residence time. The LNP's physicochemical properties improve FTR's antiretroviral activities, which are linked to the drug's ability to withstand fluid flow forces and levels of drug cellular internalization. Each is, in measure, dependent on PEGylated lipid composition and flow rate ratios affecting the size, polydispersity, shape, zeta potential, stability, biodistribution, and antiretroviral efficacy. The FTR LNP physicochemical properties enable the drug-particle's extended actions.

Publication types

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

MeSH terms

  • Animals
  • Anti-HIV Agents / administration & dosage
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacokinetics
  • Anti-HIV Agents / pharmacology
  • Delayed-Action Preparations
  • HIV Infections / drug therapy
  • HIV Infections / virology
  • HIV-1 / drug effects
  • Humans
  • Lipids / chemistry
  • Liposomes
  • Mice
  • Morpholines* / chemistry
  • Morpholines* / pharmacokinetics
  • Morpholines* / pharmacology
  • Nanoparticles* / chemistry
  • Organophosphates* / chemistry
  • Organophosphates* / pharmacokinetics
  • Organophosphates* / pharmacology
  • Piperazines
  • Tissue Distribution

Substances

  • fostemsavir
  • Organophosphates
  • Morpholines
  • Lipids
  • Lipid Nanoparticles
  • Delayed-Action Preparations
  • Anti-HIV Agents
  • Liposomes
  • Piperazines