Synthesis of pro-prodrugs L-lysine based for 5-aminosalicylic acid and 6-mercaptopurine colon specific release.

摘要: Abstract The aim of this work is to design, prepare and characterize l -lysine based prodrugs capable targeting 6-mercaptopurine the colon, an anti-tumor immunosuppressant drug, 5-aminosalicylic acid (5-ASA), drug choice for inflammatory bowel disease (IBD). More specifically, Nɛ-feruloyl-S-(6-purinyl)- Nɛ-acryloyl-S-(6-purinyl)- were synthesized then characterized by FT-IR, 1H-NMR GC/MS spectroscopies. ability feruloyl derivative in inhibiting lipid peroxidation rat liver microsomal membranes, induced vitro tert-butyl hydroperoxide as source free radicals, was evaluated. Moreover, -lysine, polymerizable prodrug, used microspheres realization 5-ASA release. These lasts, obtained emulsion inverse technique, light scattering scanning electron microscopy (SEM) analysis. equilibrium swelling degree evaluated showed good behaviour simulating colonic fluids. Results confirm possibility that application range prodrug can be extended treatment intestinal diseases whose conventional therapy envisages medications with serious side effects that, thanks new strategy, minimized optimal way.