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Synthesis and in vitro stability of amino acid prodrugs of 6-β-naltrexol for microneedle-enhanced transdermal delivery

A small library of amino acid ester prodrugs of 6-β-naltrexol (NTXOL, 1) was prepared in order to investigate the candidacy of these prodrugs for microneedle-enhanced transdermal delivery. Six amino acid ester prodrugs were synthesized (6a-f). 6b, 6d, and 6e were stable enough at skin pH (pH 5.0) to...

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Publicado en:Bioorg Med Chem Lett
Main Authors: Eldridge, Joshua A., Milewski, Mikolaj, Stinchcomb, Audra L., Crooks, Peter A.
Formato: Artigo
Idioma:Inglês
Publicado: 2014
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Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC4254627/
https://ncbi.nlm.nih.gov/pubmed/25442314
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2014.09.072
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