Anti-HIV Effect of Liposomes Bearing CXCR4 Receptor Antagonist N15P

  • Y Zhao
  • H Sun
  • X Li
  • X Mo
  • G Zhang
Keywords: Antagonist, CXCR4, Liposomes, Receptor, Inflammation, HIV


Purpose: To evaluate lymphatic system targeting and inhibitory ability of N15P nano-liposomal preparation (naLipo-N15P) of CXCR4 receptor antagonist in HIV infection.
Methods: Chemotactic and chemotaxic inhibition activity assays were used to analyze the biological activity of naLipo-N15P. The anti-HIV potential of NaLipo-N15P in vitro was evaluated when NaLipo- N15P combined with the peripheral blood mononuclear cells of Macaca fascicularis which carry the Simian immunodeficiency virus. Furthermore, the anti-HIV potential in vivo of NaLipo-N15P was evaluated by the plasma concentration and tissue distribution (Ki)
Results: The half-maximal inhibitory concentration of naLipo-N15P binding to CXCR4 as an antagonist in competition with SDF-1α was 1.89 pM while Ki was 2.4 pM. Viral load was 289 ± 45. NaLipo- N15P majorly accumulated in liver and spleen.
Conclusion: When N15P is encapsulated into nano-liposomes, it not only retains specific binding to CXCR4 and facilitates cell-type-specific targeting of nano-liposomes to PBMCs with high CXCR4 expression, but also shows enhanced anti-HIV effect. Therefore, we propose that naLipo-N15P as a CXCR4 antagonist will play an important role in inflammation and blocking of HIV infection.

Keywords: Antagonist, CXCR4, Liposomes, Receptor, Inflammation, HIV


Journal Identifiers

eISSN: 1596-9827
print ISSN: 1596-5996