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A long acting nanoformulated lamivudine ProTide.
Smith, Nathan; Bade, Aditya N; Soni, Dhruvkumar; Gautam, Nagsen; Alnouti, Yazen; Herskovitz, Jonathan; Ibrahim, Ibrahim M; Wojtkiewicz, Melinda S; Dyavar Shetty, Bhagya Laxmi; McMillan, JoEllyn; Gendelman, Howard E; Edagwa, Benson.
Afiliação
  • Smith N; Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
  • Bade AN; Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
  • Soni D; Department of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
  • Gautam N; Department of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
  • Alnouti Y; Department of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
  • Herskovitz J; Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
  • Ibrahim IM; Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
  • Wojtkiewicz MS; Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
  • Dyavar Shetty BL; Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
  • McMillan J; Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
  • Gendelman HE; Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, 68198, USA; Department of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, 68198, USA. Electronic address: hegendel@unmc.edu.
  • Edagwa B; Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, 68198, USA. Electronic address: benson.edagwa@unmc.edu.
Biomaterials ; 223: 119476, 2019 12.
Article em En | MEDLINE | ID: mdl-31525692
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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Monócitos / Infecções por HIV / Lamivudina / Fármacos Anti-HIV / Macrófagos Limite: Animals / Humans Idioma: En Revista: Biomaterials Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Monócitos / Infecções por HIV / Lamivudina / Fármacos Anti-HIV / Macrófagos Limite: Animals / Humans Idioma: En Revista: Biomaterials Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Estados Unidos