Fattahi Ali, Karimi Nadia, Rahmati Fatemeh, Shokoohinia Yalda, Sadrjavadi Komail
Medical Biology Research Center, Kermanshah University of Medical Sciences Kermanshah Iran.
Department of Chemistry, Basic of Sciences Faculty, Ilam University Ilam Iran.
RSC Adv. 2018 Apr 6;8(23):12951-12959. doi: 10.1039/c8ra01407h. eCollection 2018 Apr 3.
In the present study, camptothecin grafted poly amino ester-methyl ether polyethylene glycol (CPT-PEA-MPEG) as a novel copolymer was synthesized by Michael reaction at different ratios of MPEG and CPT (60 : 40 and 80 : 20). The microemulsion was used to prepare nanomicelles, and cytotoxicity was performed on the HT29 cell line, and cell survival was measured by MTT assay. The syntheses were confirmed by H NMR and FT-IR. Several characterization methods including CMC, particle size, size distribution, and transmission electron microscopy were performed to evaluate features of prepared nanomicelles. Low critical micelle concentration, small particle size and IC of 0.1 mg ml at MPEG to CPT ratio of 60 : 40 make this micelle a promising drug delivery carrier. CPT-PAE-MPEG nanomicelles at a MPEG : CPT ratio of 60 : 40 can be a suitable choice to improve the physiochemical properties of CPT and its therapeutic effect, while it can be potentially used as a nano-carrier for other anticancer drugs to purpose a dual drug delivery.
在本研究中，通过迈克尔反应以不同比例的甲氧基聚乙二醇（MPEG）和喜树碱（CPT）（60∶40和80∶20）合成了喜树碱接枝的聚氨基酯-甲基醚聚乙二醇（CPT-PEA-MPEG）这种新型共聚物。使用微乳液制备纳米胶束，并在HT29细胞系上进行细胞毒性实验，通过MTT法测定细胞存活率。通过氢核磁共振（H NMR）和傅里叶变换红外光谱（FT-IR）对合成产物进行了确认。采用了包括临界胶束浓度（CMC）、粒径、粒径分布和透射电子显微镜等多种表征方法来评估所制备纳米胶束的特性。在MPEG与CPT比例为60∶40时，临界胶束浓度低、粒径小且半数抑制浓度（IC）为0.1mg/ml，使得这种胶束成为一种有前景的药物递送载体。MPEG∶CPT比例为60∶40的CPT-PAE-MPEG纳米胶束可能是改善喜树碱理化性质及其治疗效果的合适选择，同时它有可能作为其他抗癌药物的纳米载体用于双重药物递送。
