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.