Synthesis, characterization and in vitro studies of pegylated melphalan conjugates

摘要: Melphalan, a drug used for the treatment of breast, ovaries and certain type cancer in bone marrow, was conjugated to linear methoxy poly (ethylene glycol) (M-PEG) 2000 5000, Da. An ester linkage between polymer coupling yield polymeric prodrug. Purified esters were characterized by Maldi-Tof IR spectroscopy methods. The modification allowed overcoming known melphalan aqueous solubility problem (0.1 µg/ml) leading us obtain polymer-drug bioconjugate more suitable oral parental administration. It found that molecular weight M-PEG is critical conjugates stability, (80 times 123 higher respectively), hemolytic activity. caused 100% hemolysis above concentration 3.5 µg/ml 1 h. whereas conjugate 5000 shows 81.3 ± 0.5% 48.8 ± 1.5% hemolysis, respectively at 32 after1 h. Further In vitro anticanc...