Melphalan-loaded methoxy poly(ethylene glycol)-poly(D,L-lactide)copolymer nanomicelles in the treatment of multiple myeloma  

作　　者：Yingying Chen Qiang Zeng Bingyang Chu Zhigang Liu Xue Wei Mengran Chen Peipei Yang Minghai Tang Ting Niu Yongqian Jia Ying Qu Zhiyong Qian 

机构地区：[1]Department of Hematology and Institute of Hematology,State Key Laboratory of Biotherapy,West China Hospital,Sichuan University,Chengdu 610041,China

出　　处：《Chinese Chemical Letters》2023年第9期193-198,共6页中国化学快报（英文版）

基　　金：supported by the National Natural Science Foundation of China(Nos.U21A20417,31930067,32271450,31700868);PostDoc Research Project,West China Hospital,Sichuan University(No.2020HXBH165);1·3·5 Project for Disciplines of Excellence,West China Hospital,Sichuan University(No.ZYGD18002)。

摘　　要：Multiple myeloma(MM)is the second most common hematological tumor characterized by the proliferation of monoclonal plasma cells.Melphalan(MEL)is commonly used in the treatment of MM and is especially essential for patients undergoing autologous stem cell transplantation(ASCT).Although many drugs for MM have been developed in recent years,chemotherapy followed by ASCT remains the optimal option.Melphalan,the backbone of the conditioning regimen,brings severe toxicities at a high dose.Nanodrug delivery systems enable drugs to be highly effective and have low toxicity.In this study,methoxy poly(ethylene glycol)-poly(D,L-lactide)copolymer(MPEG-PDLLA)was chosen to encapsulate melphalan,and the characteristics,effectiveness,and safety of MEL/MPEG-PDLLA in vitro and in vivo were investigated.MEL/MPEG-PDLLA showed slow release and was easily engulfed by MM cells despite a result of the antitumor assay comparable to that of free melphalan in vitro.The in vivo results showed that MEL/MPEG-PDLLA could significantly alleviate tumor burden and prolong survival time without increasing the toxicity to vital organs.In addition,MEL/MPEG-PDLLA could significantly reduce the damage to the intestinal mucosa caused by melphalan.In conclusion,MEL/MPEG-PDLLA shows improved antitumor activity and has the potential to alleviate pains of MM patients undergoing ASCT.

关 键 词：MELPHALAN Multiple myeloma MPEG-PDLLA Nanomicelle 

分 类 号：R733.3[医药卫生—肿瘤] TB383.1[医药卫生—临床医学]