Membrane-associated drug transporters are important determinants of antiretroviral drug disposition in the central nervous system
during HIV-1 infection. A number of influx and efflux transport proteins expressed at the blood-brain barrier, blood-cerebrospinal
fluid barrier and in brain parenchyma cellular compartments (i.e., astrocytes, microglia) have been implicated in the traffic of many
antiretroviral drugs into and out of the brain. In particular, members of the ATP-binding cassette membrane associated transporter superfamily
and Solute Carrier family are known to be involved in the efflux and/or influx of drugs, respectively. As a result, changes in the
functional expression of these transporters can alter the disposition and distribution of drugs in the brain. Moreover, antiretroviral therapy
itself and/or pathological events (i.e., inflammation, oxidative stress) associated with viral infection may affect the functional expression
of these transporters. This review summarizes recent knowledge on the role of drug transporters in regulating brain antiretroviral drug
transport in the context of HIV-1 infection.
Keywords: HIV-1, brain, drug transport, ABC transporter, SLC transporter, antiretroviral drugs, neuropathogenesis.
Rights & PermissionsPrintExport