Abstract
Novel glycerolipidic prodrugs of didanosine and didanosine monophosphate designed to by-pass the hepatic first pass metabolism were synthesized and tested for their cytotoxicity and anti-HIV-1 activity. Formulation as liposomes of dipalmitoylphosphatidylcholine was elaborated. A simple quantitative HPLC-UV method was developed and validated, and ESI-MS was used for qualitative purpose. These two prodrugs exhibited promising biological activities against HIV-1 in in vitro infected cell culture.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-HIV Agents / administration & dosage
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Anti-HIV Agents / chemical synthesis*
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Anti-HIV Agents / pharmacokinetics*
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Biological Availability
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Cells, Cultured
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Didanosine / administration & dosage
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Didanosine / chemical synthesis*
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Didanosine / pharmacokinetics*
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Drug Delivery Systems / methods*
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Humans
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Leukocytes, Mononuclear / drug effects
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Leukocytes, Mononuclear / virology
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Liposomes
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Lymphatic System / metabolism*
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Lymphatic System / virology
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Prodrugs / chemical synthesis*
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Prodrugs / pharmacokinetics*
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Purine Nucleosides / administration & dosage
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Purine Nucleosides / therapeutic use
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Triglycerides / chemical synthesis*
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Triglycerides / pharmacokinetics*
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Virus Replication / drug effects
Substances
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Anti-HIV Agents
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Liposomes
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Prodrugs
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Purine Nucleosides
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Triglycerides
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Didanosine