Lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir

Here, the authors provide a mechanism for an improved version of a nanoformulated myristoylated prodrug of cabotegravir (CAB), named NM2CAB, and its bioavailability, stability and pharmacokinetics in mice and rats performed in independent academic and a contracted research labs, suggesting that the...

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Autores principales: Nagsen Gautam, JoEllyn M. McMillan, Devendra Kumar, Aditya N. Bade, Qiaoyu Pan, Tanmay A. Kulkarni, Wenkuan Li, Brady Sillman, Nathan A. Smith, Bhagya L. Dyavar Shetty, Adam Szlachetka, Benson J. Edagwa, Howard E. Gendelman, Yazen Alnouti
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Publicado: Nature Portfolio 2021
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Acceso en línea:https://doaj.org/article/2bfe8aa999a043d6aa5d494a5ae8099d
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spelling oai:doaj.org-article:2bfe8aa999a043d6aa5d494a5ae8099d2021-12-02T14:58:13ZLipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir10.1038/s41467-021-23668-x2041-1723https://doaj.org/article/2bfe8aa999a043d6aa5d494a5ae8099d2021-06-01T00:00:00Zhttps://doi.org/10.1038/s41467-021-23668-xhttps://doaj.org/toc/2041-1723Here, the authors provide a mechanism for an improved version of a nanoformulated myristoylated prodrug of cabotegravir (CAB), named NM2CAB, and its bioavailability, stability and pharmacokinetics in mice and rats performed in independent academic and a contracted research labs, suggesting that the extended half-life of the prodrug is not a property of enzymatic hydrolysis but rather release or dissolution of the prodrug from the nanocrystal.Nagsen GautamJoEllyn M. McMillanDevendra KumarAditya N. BadeQiaoyu PanTanmay A. KulkarniWenkuan LiBrady SillmanNathan A. SmithBhagya L. Dyavar ShettyAdam SzlachetkaBenson J. EdagwaHoward E. GendelmanYazen AlnoutiNature PortfolioarticleScienceQENNature Communications, Vol 12, Iss 1, Pp 1-13 (2021)
institution DOAJ
collection DOAJ
language EN
topic Science
Q
spellingShingle Science
Q
Nagsen Gautam
JoEllyn M. McMillan
Devendra Kumar
Aditya N. Bade
Qiaoyu Pan
Tanmay A. Kulkarni
Wenkuan Li
Brady Sillman
Nathan A. Smith
Bhagya L. Dyavar Shetty
Adam Szlachetka
Benson J. Edagwa
Howard E. Gendelman
Yazen Alnouti
Lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir
description Here, the authors provide a mechanism for an improved version of a nanoformulated myristoylated prodrug of cabotegravir (CAB), named NM2CAB, and its bioavailability, stability and pharmacokinetics in mice and rats performed in independent academic and a contracted research labs, suggesting that the extended half-life of the prodrug is not a property of enzymatic hydrolysis but rather release or dissolution of the prodrug from the nanocrystal.
format article
author Nagsen Gautam
JoEllyn M. McMillan
Devendra Kumar
Aditya N. Bade
Qiaoyu Pan
Tanmay A. Kulkarni
Wenkuan Li
Brady Sillman
Nathan A. Smith
Bhagya L. Dyavar Shetty
Adam Szlachetka
Benson J. Edagwa
Howard E. Gendelman
Yazen Alnouti
author_facet Nagsen Gautam
JoEllyn M. McMillan
Devendra Kumar
Aditya N. Bade
Qiaoyu Pan
Tanmay A. Kulkarni
Wenkuan Li
Brady Sillman
Nathan A. Smith
Bhagya L. Dyavar Shetty
Adam Szlachetka
Benson J. Edagwa
Howard E. Gendelman
Yazen Alnouti
author_sort Nagsen Gautam
title Lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir
title_short Lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir
title_full Lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir
title_fullStr Lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir
title_full_unstemmed Lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir
title_sort lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir
publisher Nature Portfolio
publishDate 2021
url https://doaj.org/article/2bfe8aa999a043d6aa5d494a5ae8099d
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