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Self-Assembled Nanoparticles Platform Based on Pectin-Dihydroartemisinin Conjugates for Codelivery of Anticancer Drugs
ACS Biomaterials Science & Engineering ( IF 5.4 ) Pub Date : 2017-11-20 00:00:00 , DOI: 10.1021/acsbiomaterials.7b00842
Yanxue Liu 1 , Dan Zheng 1 , Yunyun Ma 1 , Juan Dai 1 , Chunxiao Li 1 , Shangzhen Xiao 1 , Kefeng Liu 1 , Jing Liu 1 , Luying Wang 1 , Jiandu Lei 1 , Jing He 1
Affiliation  

Natural pectin is an important carrier for delivering drugs in biomedical research, however, there are only a few reports on the preparation of pectin nanoparticles, especially a particle size of below 100 nm with high yield. Here we design pectin-dihydroartemisinin/hydrooxycampothecin nanoparticles (PDC-H NPs) through a self-assembly method. The prepared PDC-H NPs contained hydrophilic part of pectin and hydrophobic anticancer drugs of dihydroartemisinin and hydroxycamptothecin, which could increase drug loading, improve water solubility, and achieve controlled release of drugs. The results indicated that the particle size of PDC-H NPs was about 70 nm, drug-loaded efficiency of DHA was 20.33 wt %, and encapsulation efficiency of HCPT was 14.11 wt %. PDC-H NPs exhibited a higher cytotoxicity, the blood retention time of PDC-H NPs was 4.8-fold longer than DHA and was 6.8-fold longer than HCPT. In addition, effective cellular uptake exhibited an obvious synergistic effect compared with DHA and HCPT. 4T1 tumor-bearing mice also showed a higher survival rate than free DHA and free HCPT. The result show that the self-assembled PDC-H NPs is a promising anticancer drug for codelivery.

中文翻译:

基于果胶-双氢青蒿素的自组装纳米粒子平台共轭抗癌药物的代码传递。

天然果胶是生物医学研究中传递药物的重要载体,但是,关于果胶纳米颗粒制备的报道很少,尤其是粒径高至100 nm以下的果胶。在这里,我们通过自组装方法设计果胶-二氢青蒿素/羟基喜树碱纳米粒子(PDC-H NPs)。制备的PDC-H NPs含有果胶的亲水性部分,双氢青蒿素和羟基喜树碱的疏水性抗癌药,可以增加载药量,改善水溶性,实现药物的控释。结果表明,PDC-H NPs的粒径约为70 nm,DHA的载药效率为20.33 wt%,HCPT的包封效率为14.11 wt%。PDC-H NPs具有较高的细胞毒性,PDC-H NPs的血液保留时间为4。比DHA长8倍,比HCPT长6.8倍。另外,与DHA和HCPT相比,有效的细胞摄取表现出明显的协同作用。携带4T1肿瘤的小鼠还显示出比游离DHA和游离HCPT高的存活率。结果表明,自组装的PDC-H NPs是一种有希望的代码传递抗癌药物。
更新日期:2017-11-20
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