Related Experiment Video
Updated: Jul 6, 2026

Development of Cell-type specific anti-HIV gp120 aptamers for siRNA delivery
Published on: June 23, 2011
Interactions of pluronic block copolymers on P-gp efflux activity: experience with HIV-1 protease inhibitors
Naveed Shaik1, Guoyu Pan, William F Elmquist
1Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 308 Harvard St. SE, Room 9-125d, Weaver-Densford Hall, Minneapolis, Minnesota 55455, USA.
Abstract:
The objective was to examine the influence of Pluronic block-copolymers on the interaction between the drug efflux transporter, P-glycoprotein and HIV-1 protease inhibitors (PIs). The ATPase assay determined the effect of various Pluronics on PI-stimulated P-gp ATPase activity. Cellular accumulation studies were conducted using MDCKII and LLC-PK1 cells transfected with human MDR1 to assess Pluronic modulation of PI efflux. Pluronic P85 inhibited both basal and nelfinavir-stimulated P-gp ATPase activity, while Pluronic F127 had no effect. In cell accumulation studies, Pluronic P85 restored the accumulation of nelfinavir in MDCKII-MDR1 cells while Pluronic F127 and F88 had no effect. Pluronic P85 increased saquinavir accumulation in wild-type and MDR1-transfected cells in both the MDCKII and LLC-PK1 cell models, suggesting inhibition of multiple transporters, including MRPs. In conclusion, this study provides evidence that a block-copolymer, Pluronic P85, effectively inhibits the interaction of P-gp with nelfinavir and saquinavir. These data indicate that effective inhibition of HIV-1 PI efflux by Pluronic P85 may influence the distribution of antiretroviral agents to sites protected by efflux mechanisms, such as the blood-brain barrier, and possibly increase the brain exposure of these drugs resulting in suppression of viral replication and reduction in the incidence of drug resistant mutants.
Related Concept Videos
Inhibitors of Virion Maturation and Assembly
Pharmacokinetics: Drug–Food and Drug–Viral Interactions
Factors Affecting Protein-Drug Binding: Drug Interactions
Displacement interactions can have varying outcomes, ranging from toxicity to virtually...
Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters
Depolarizing Blockers: Pharmocokinetics
Inhibitors of Viral Protein Synthesis

