Lipid–drug conjugates and associated carrier strategies for enhanced antiretroviral drug delivery

Abstract

Mortality rate of patients infected with HIV-1 has been significantly reduced by using HAART. However, the virus to date has not been eradicated. Transmission of HIV-1 infection through sexual intercourse remains an ongoing challenge, with increased risk of infection occurring in women. Interestingly, ARV drugs can be chemically linked with lipids to produce lipid–drug conjugates (LDCs). This alters pharmacokinetic properties of ARV drugs and thereby resulting in improved effectiveness. Although LDCs can be administered without a delivery carrier, they are usually incorporated into suitable delivery systems such as lipid nanoparticles, polymeric nanoparticles, micelles, liposomes, emulsions, and carbon nanotubes. Given that LDCs have the potential to improve oral bioavailability, lipophilicity, toxicity, and drug targeting, it is of our great interest to review strategies of lipid–drug conjugation together with their delivery systems for enhanced antiretroviral efficacy.

Keywords:

• HIV-1
• antiretrovirals
• lipid–drug conjugates
• drug delivery
• nanoparticles

Disclosure statement

The authors confirm that there is no conflict of interest.

Additional information

Funding

This work was funded by the National Research Foundation (NRF) and the South African Medical Research Council (SAMRC).