Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Anti-HIV Effect of Liposomes Bearing CXCR4 Receptor Antagonist N15P

Yingxia Zhao, Hanxiao Sun , Xiuying Li, Xuemei Mo, Guang Zhang

College of Pharmacy, Jinan UniversityA292;GuangZhouA292;GuangDong ProvinceA292;ChinaA292;510632;

For correspondence:- Hanxiao Sun Email: fangcaobi860317@163.com Tel:+8615201543769

Received: 22 June 2013 Accepted: 28 July 2013 Published: 23 August 2013

Citation: Zhao Y, Sun H, Li X, Mo X, Zhang G. Anti-HIV Effect of Liposomes Bearing CXCR4 Receptor Antagonist N15P. Trop J Pharm Res 2013; 12(4):503-509 doi: 10.4314/tjpr.v12i4.9

© 2013 The authors.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..

Abstract

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