ArticleACS applied materials & interfaces2025
Rilpivirine Ionic Liquid Nanoemulsion Augments the Oral Bioavailability of Rilpivirine and Its Delivery to the HIV Sanctuary Sites.
Article in ACS applied materials & interfaces, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Rilpivirine (RPV) is a potent antiretroviral drug used for the long-term management of HIV infection. The high crystallinity and very low aqueous solubility of RPV are responsible for the highly variable pharmacokinetics of RPV seen in HIV-infected patients. While fatty meals can increase the absorption of RPV, the low lipid solubility of RPV precludes the development of oral lipid-based formulations such as self-nanoemulsifying systems (SNES). To improve the oral delivery of RPV, we evaluated the potential of six biocompatible bulky anions to transform RPV into amphiphilic RPV ionic liquids with high lipid solubility and only sodium docusate successfully yielded an amphiphilic RPV ionic liquid (IL), RPV docusate (RPV-Doc). Spectroscopic, chromatographic, and thermal characterization techniques confirmed the formation of RPV-Doc as an IL. RPV-Doc showed remarkably higher (∼100-200-fold) solubility in lipids compared to pure RPV. RPV-Doc was incorporated into two SNES formulations that, depending upon the composition of the SNES formulation, yielded a <100 or <250 nm nanoemulsion irrespective of the pH of the dilution medium. Oral pharmacokinetics and biodistribution studies in mice showed that both SNES formulations containing RPV-Doc yielded rapid and significantly higher oral bioavailability (∼6-fold higher
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