A long acting nanoformulated lamivudine ProTide.
basic_science · Level V
Where this comes from
- Record sourced from PubMed, PMID 31525692.
- Also identified by DOI 10.1016/j.biomaterials.2019.119476 and PMC identifier 6945491.
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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<sup>+</sup> 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.
Medical subject headings
- Anti-HIV Agents
- HIV Infections
- Lamivudine
- Macrophages
- Monocytes