Ketoprofen-polyethylene glycol conjugate: synthesis, kinetic study on hydrolysis and the formation of micelle

摘要

Ketoprofen (KP), a potent analgesic and non-steroidal anti-inflammatory drug (NSAID), has been widely used in the treatment of rheumatoid arthristis and its related conditions. However, KP has some disadvantages, such as relatively short half-life (1.5-4 hour) in plasma, irritation of gastrointestinal tract and ulceration/hemorrhage~1. In order to minimise these disadvantages, numerous esters of KP have been prepared and tested for their gastrointestinal irritation and anti-inflammatory effect~2,3. In this work, we have prepared a KP prodrug, KP-polyethylene glycol (PEG) conjugate (KPEG), and studied its kinetics of hydrolysis. The solution behaviour of KPEG was also studied using dynamic light scattering. and the critical micelle concentration (CMC) was determined.