培美曲塞纳米制剂研究进展

Research progress of Pemetrexed nanoformulation

培美曲塞(PEM)是对叶酸代谢途径多靶点阻断的新一代抗肿瘤药,疗效高于其他传统抗叶酸类药物。但由于该药缺乏肿瘤特异性,存在剂量依赖性毒副作用,导致其临床应用受限。纳米载体由于靶向给药策略在降低毒性和改善治疗效果方面具有独特的优势而受到广泛关注。近年来,关于PEM的纳米制剂研究,包括脂质体、纳米粒、胶束、纳米乳、水凝胶等,在提高PEM的溶解度、延长体内循环时间、提高靶向性、降低不良反应、增强抗肿瘤活性等方面取得一定进展,并开发出不同的给药方式。本文对PEM纳米制剂研究进展进行综述,为PEM新型纳米制剂的开发和应用提供理论依据。

Pemetrexed(PEM)is a new generation of anti-tumor drug that blocks multiple targets of folate metabolism pathway,and it is more effective than other traditional anti-folate drugs.However,due to the lack of tumor specificity and dose-dependent toxicity,its clinical application is limited.Nanocarriers have attracted wide attention because of their unique advantages in reducing toxicity and improving therapeutic effect.In recent years,studies on PEM nanoparticles,including liposomes,nanoparticles,micelles,nanoemulsions and hydrogels,have made some progress in improving the solubility of PEM,prolonging the circulation time in vivo,improving targeting,reducing adverse reactions and enhancing anti-tumor activity,and different drug delivery methods have been developed.This paper reviews the research progress of PEM nanopreparation,and provides the theoretical basis for the development and application of new PEM nanopreparation.