Studies On LXT-101 Sustained-release Injectable Microspheres To Treat Prostate Cancer

More and more peptides and proteins become main and important drugs along with the progress of genomics and proteomics. However, compared with low molecular weight drugs, the distinct properties of them, such as easy degradation (e.g. by deamidation, oxidation and hydrolysis), instability, low bioavailability and short half lives, make traditional dosage forms not proper to deliver them. So it's a significant task to deliver proteins and peptides to target organs and tissues. Nowadays the biopharmaceutical drugs on clinical use are supplied as sterile freeze-dried powder or injectable solutions. These formulations mentioned above are administerd frequently and this makes the patients' compliance poor and the therapy cost high. However, if they would be incorporated into the biodegradable sustained-release injectable microspheres, it could prevent the biopharmaceutical drugs from eliminating rapidly and prolonged the administration interval. In addition the advantages include: (1) maintaining minimum effective concentration and avoiding the peak-valley phenomenon which appeared regularly in the common formulations; (2) decreasing total dose and alleviating some toxic and adverse actions. Therefore, biodegradable sustained-release injectable microspheres have been studied extensively in the last two decades in the pharmaceutical field.Poly(DL-lactide) (PLA) and poly(DL-lactide-co-glycolide) (PLGA) have been sanctioned by FDA as drugs additive due to their good biodegradable and biocompatible properties. LXT-101 is the second generation of luteinizing hormone-releasing hormone (LHRH) antagonists. The major advantage of LHRH antagonists (such as cetrorelix,...