Xue Ziyang, Fu Rongzhan, Duan Zhiguang, Chi Lei, Zhu Chenhui, Fan Daidi
Shaanxi Key Laboratory of Degradable Biomedical Materials and Shaanxi R&D Center of Biomaterials and Fermentation Engineering, School of Chemical Engineering, Northwest University, Taibai North Road 229, Xi'an 710069, China.
Biotech & Biomed Research Institute, Northwest University, Taibai North Road 229, Xi'an 710069, China.
Polymers (Basel). 2021 May 28;13(11):1784. doi: 10.3390/polym13111784.
Ginsenoside CK is one of the intestinal bacterial metabolites of ginsenoside prototype saponins, such as ginsenoside Rb1, Rb2, Rc, and Rd. Poor water solubility and low bioavailability have limited its application. The nanogel carriers could specifically deliver hydrophobic drugs to cancer cells. Therefore, in this study, a nanogel was constructed by the formation of Schiff base bonds between hydrazide-modified carboxymethyl cellulose (CMC-NH) and aldehyde-modified β-cyclodextrin (β-CD-CHO). A water-in-oil reverse microemulsion method was utilized to encapsulate ginsenoside CK via the hydrophobic cavity of β-CD. β-CD-CHO with a unique hydrophobic cavity carried out efficient encapsulation of CK, and the drug loading and encapsulation efficiency were 16.4% and 70.9%, respectively. The drug release of CK-loaded nanogels (CK-Ngs) in vitro was investigated in different pH environments, and the results showed that the cumulative release rate at pH 5.8 was 85.5% after 140 h. The methylthiazolyldiphenyl-tetrazolium bromide (MTT) toxicity analysis indicated that the survival rates of A549 cells in CK-Ngs at 96 h was 2.98% compared to that of CK (11.34%). In vivo animal experiments exhibited that the inhibitory rates of CK-Ngs against tumor volume was 73.8%, which was higher than that of CK (66.1%). Collectively, the pH-responsive nanogel prepared herein could be considered as a potential nanocarrier for CK to improve its antitumor effects against lung cancer.
人参皂苷CK是人参皂苷原型皂苷（如人参皂苷Rb1、Rb2、Rc和Rd）的肠道细菌代谢产物之一。其水溶性差和生物利用度低限制了其应用。纳米凝胶载体可以将疏水性药物特异性递送至癌细胞。因此，在本研究中，通过酰肼修饰的羧甲基纤维素（CMC-NH）与醛修饰的β-环糊精（β-CD-CHO）之间形成席夫碱键构建了一种纳米凝胶。采用油包水反相微乳液法通过β-环糊精的疏水腔包封人参皂苷CK。具有独特疏水腔的β-CD-CHO对CK进行了有效包封，载药量和包封率分别为16.4%和70.9%。研究了载人参皂苷CK纳米凝胶（CK-Ngs）在不同pH环境下的体外药物释放情况，结果表明，在pH 5.8时，140 h后的累积释放率为85.5%。甲基噻唑基二苯基四氮唑溴盐（MTT）毒性分析表明，与CK组（11.34%）相比，96 h时CK-Ngs组A549细胞的存活率为2.98%。体内动物实验表明，CK-Ngs对肿瘤体积的抑制率为73.8%，高于CK组（66.1%）。总体而言，本文制备的pH响应性纳米凝胶可被视为一种潜在的CK纳米载体，以提高其对肺癌的抗肿瘤作用。
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