Chen Xuelian, Liu Lijia, Shen Chen, Liu Fangyan, Xu Enyu, Chen Yin, Jie Wang
College of Food and Pharmacy, Zhejiang Ocean University, Zhoushan 316000, China.
Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China.
Polymers (Basel). 2023 May 30;15(11):2510. doi: 10.3390/polym15112510.
In recent years, natural polysaccharides have been widely used in the preparation of drug delivery systems. In this paper, novel polysaccharide-based nanoparticles were prepared by layer-by-layer assembly technology using silica as a template. The layers of nanoparticles were constructed based on the electrostatic interaction between a new pectin named NPGP and chitosan (CS). The targeting ability of nanoparticles was formed by grafting the RGD peptide, a tri-peptide motif containing arginine, glycine, and aspartic acid with high affinity to integrin receptors. The layer-by-layer assembly nanoparticles (RGD-(NPGP/CS)NPGP) exhibited a high encapsulation efficiency (83.23 ± 6.12%), loading capacity (76.51 ± 1.24%), and pH-sensitive release property for doxorubicin. The RGD-(NPGP/CS)NPGP nanoparticles showed better targeting to HCT-116 cells, the integrin αvβ3 high expression human colonic epithelial tumor cell line with higher uptake efficiency than MCF7 cells, the human breast carcinoma cell line with normal integrin expression. In vitro antitumor activity tests showed that the doxorubicin-loaded nanoparticles could effectively inhibit the proliferation of the HCT-116 cells. In conclusion, RGD-(NPGP/CS)NPGP nanoparticles have potential as novel anticancer drug carriers because of their good targeting and drug-carrying activity.
近年来,天然多糖已广泛应用于药物递送系统的制备。本文以二氧化硅为模板,采用层层组装技术制备了新型多糖基纳米粒子。纳米粒子层是基于一种名为NPGP的新型果胶与壳聚糖(CS)之间的静电相互作用构建而成。通过接枝RGD肽(一种对整合素受体具有高亲和力的包含精氨酸、甘氨酸和天冬氨酸的三肽基序)形成纳米粒子的靶向能力。层层组装纳米粒子(RGD-(NPGP/CS)NPGP)对阿霉素表现出高包封率(83.23±6.12%)、载药量(76.51±1.24%)和pH敏感释放特性。RGD-(NPGP/CS)NPGP纳米粒子对HCT-116细胞表现出更好的靶向性,HCT-116细胞是整合素αvβ3高表达的人结肠上皮肿瘤细胞系,其摄取效率高于MCF7细胞(整合素表达正常的人乳腺癌细胞系)。体外抗肿瘤活性测试表明,载有阿霉素的纳米粒子能有效抑制HCT-116细胞的增殖。总之,RGD-(NPGP/CS)NPGP纳米粒子因其良好的靶向性和载药活性而具有作为新型抗癌药物载体的潜力。