Antiretroviral Solid Drug Nanoparticles with Enhanced Oral Bioavailability: Production, Characterization, and In Vitro–In Vivo Correlation (pages 400–411)
Tom O. McDonald, Marco Giardiello, Philip Martin, Marco Siccardi, Neill J. Liptrott, Darren Smith, Phill Roberts, Paul Curley, Alessandro Schipani, Saye H. Khoo, James Long, Alison J. Foster, Steven P. Rannard and Andrew Owen
Article first published online: 1 SEP 2013 | DOI: 10.1002/adhm.201300280
Emulsion-templated freeze-drying to form solid drug nanoparticles is applied for the first time to the optimization of oral HIV therapies. A solid formulation with 70 wt% efavirenz is optimized and shown to have considerable long-term stability in the amorphous state, with lower cytotoxicity and higher in vivo oral bioavailability than conventional formulations. The results offer a reduced daily drug dose and the first oral HIV nanomedicine.