@article{9815d5975b7b4b89aaa0c2c788882de4,
title = "A long acting nanoformulated lamivudine ProTide",
abstract = "A long acting (LA) hydrophobic and lipophilic lamivudine (3TC) was created as a phosphoramidate pronucleotide (designated M23TC). M23TC improved intracellular delivery of active triphosphate metabolites and enhanced antiretroviral and pharmacokinetic (PK) profiles over the native drug. A single treatment of human monocyte derived macrophages (MDM) with nanoformulated M23TC (NM23TC) improved drug uptake, retention, intracellular 3TC triphosphates and antiretroviral activities in MDM and CD4+ T cells. PK tests of NM23TC administered to Sprague Dawley rats demonstrated sustained prodrug and drug triphosphate levels in blood and tissues for 30 days. The development of NM23TC remains a substantive step forward in producing LA slow effective release antiretrovirals for future clinical translation.",
keywords = "Antiretroviral therapy, Formulation, Lamivudine, Long-acting, ProTide, Prodrug",
author = "Nathan Smith and Bade, {Aditya N.} and Dhruvkumar Soni and Nagsen Gautam and Yazen Alnouti and Jonathan Herskovitz and Ibrahim, {Ibrahim M.} and Wojtkiewicz, {Melinda S.} and {Dyavar Shetty}, {Bhagya Laxmi} and McMillan, {Jo Ellyn} and Gendelman, {Howard E.} and Benson Edagwa",
note = "Funding Information: We wish to thank the University of Nebraska Medical Center Cores for Electron Microscopy (Tom Bargar & Nicholas Conoan), NMR Spectroscopy (Ed Ezell), Elutriation and Cell Separation (Myhanh Che and Na Ly). This research was supported by the University of Nebraska Foundation , which includes donations from the Carol Swarts, M.D. Emerging Neuroscience Research Laboratory, the Margaret R. Larson Professorship, and the Frances and Louie Blumkin and Harriet Singer Endowments, the Vice Chancellor's Office of the University of Nebraska Medical Center for Core Facility Developments, and National Institutes of Health grants R01 MH104147 , P01 DA028555 , R01 NS36126 , P01 NS31492 , 2R01 NS034239 , P01 MH64570 , P30 MH062261 , P30 AI078498 , R01 AG043540 and 1 R56 AI138613-01A1 . Publisher Copyright: {\textcopyright} 2019 Elsevier Ltd",
year = "2019",
month = dec,
doi = "10.1016/j.biomaterials.2019.119476",
language = "English (US)",
volume = "223",
journal = "Biomaterials",
issn = "0142-9612",
publisher = "Elsevier BV",
}