Rilpivirine Ionic Liquid Nanoemulsion Augments the Oral Bioavailability of Rilpivirine and Its Delivery to the HIV Sanctuary Sites

• DOI: 10.1021/acsami.5c05456
• Publication Date: 2025-05-20T14:51:25Z
• Authors: Yogesh Sutar; Joseph S. Adams; Xiangmeng Wu; Vaibhavi Bhoyarekar; Monica Garcia Diaz; Jennillee Wallace; Masumi Dave; Qing-Yu Zhang; Abhijit A. Date
• Keywords: Rilpivirine

Rilpivirine (RPV) is a potent antiretroviral drug used for the long-term management of HIV infection. The high crystallinity and very low aqueous solubility RPV are responsible highly variable pharmacokinetics seen in HIV-infected patients. While fatty meals can increase absorption RPV, lipid precludes development oral lipid-based formulations such as self-nanoemulsifying systems (SNES). To improve delivery we evaluated potential six biocompatible bulky anions to transform into amphiphilic ionic liquids with only sodium docusate successfully yielded an liquid (IL), (RPV-Doc). Spectroscopic, chromatographic, thermal characterization techniques confirmed formation RPV-Doc IL. showed remarkably higher (∼100-200-fold) lipids compared pure RPV. was incorporated two SNES that, depending upon composition formulation, <100 or <250 nm nanoemulsion irrespective pH dilution medium. Oral biodistribution studies mice that both containing rapid significantly bioavailability (∼6-fold Cmax AUC) suspension. Furthermore, suspension, resulted sustained levels sanctuary sites mesenteric lymph nodes brain. Taken together, our innovative approach be tissue penetration which eventually result reduction pharmacokinetic variability therapeutic dose leading optimal utilization.