Literature DB >> 17276686

Synthesis and biological evaluation of two glycerolipidic prodrugs of didanosine for direct lymphatic delivery against HIV.

Muriel Lalanne1, Angelo Paci, Karine Andrieux, Nathalie Dereuddre-Bosquet, Pascal Clayette, Alain Deroussent, Micheline Ré, Gilles Vassal, Patrick Couvreur, Didier Desmaële.   

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.

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Year:  2007        PMID: 17276686     DOI: 10.1016/j.bmcl.2007.01.062

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  From sewer to saviour - targeting the lymphatic system to promote drug exposure and activity.

Authors:  Natalie L Trevaskis; Lisa M Kaminskas; Christopher J H Porter
Journal:  Nat Rev Drug Discov       Date:  2015-10-16       Impact factor: 84.694

Review 2.  Intestinal lymphatic transport for drug delivery.

Authors:  Jaime A Yáñez; Stephen W J Wang; Ian W Knemeyer; Mark A Wirth; Kevin B Alton
Journal:  Adv Drug Deliv Rev       Date:  2011-06-13       Impact factor: 15.470

Review 3.  Lipid-based delivery systems and intestinal lymphatic drug transport: a mechanistic update.

Authors:  Natalie L Trevaskis; William N Charman; Christopher J H Porter
Journal:  Adv Drug Deliv Rev       Date:  2007-11-07       Impact factor: 15.470

  3 in total

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