Lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir
oleh: 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
| Format: | Article |
|---|---|
| Diterbitkan: | Nature Portfolio 2021-06-01 |
Deskripsi
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.