Magliocca, Salvatore (2015) Profarmaco: un approccio strategico in continua crescita in campo farmaceutico. Doctoral Thesis.
During my PhD course I synthesized galactosylated prodrugs of indomethacin, flurbiprofen, ketoprofen, mefenamic acid, diclofenac and ibuprofen. In the synthesis of these prodrugs, when possible, was used a ionic liquid exactly 1-butyl-3-methylimidazolium hexafluorophosphate ([bmim][PF6]) in order to reduce pollutants and improve the yields. Then for each prodrug were studied chemical and enzymatic stability (human plasma) in vitro, in order to perform pharmacological experiments in vivo. All the prodrugs showed pharmacological and toxicological profile better than parent drugs, indeed a remarkable reduction of ulcerogenicity was found. I worked also at another project aiming to enhance concentration of mycophenolic acid, an immunosuppressant, in lymphatic vessels. In this case was used 1,3-dipalmitoil diglyceride as vector linked, via different spacers, to parent drug. Lymphatic transport studies were performed on synthesized prodrugs evaluating the lymphatic concentration of parent drug; the experimental results showed that the amount of mycophenolic acid released in the lymphatic vessels by prodrugs is higher than the immunosuppressant itself.
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