Zhongyu Xu, Jiangmeng Ren, Qiufang Jing, Fuzheng Ren, Mengting Huang, Wenrui Ding, Bubing Zeng
East China University of Science and Technology Meilong Road 130 Shanghai China
RSC Adv. 2018 Oct 9;8(60):34726-34732. doi: 10.1039/c8ra04156c. eCollection 2018 Oct 4.
Andrographolide (AP) is a diterpenoid separated from with a wide spectrum of biological activities including anti-inflammatory, anticancer, hepatoprotective, and antihyperlipidemic. However, its poor water solubility and instability result in lower bioavailability, which seriously limit its pharmacological function. In this study, the attempt to use regenerated silk fibroin (RSF) as a drug-carrier to encapsulate AP was reported. The AP-loaded RSF nanoparticles were prepared by a facile and clean method without any toxic agents. Moreover, special attention was paid to the optimization of formulation. Finally, the sizes of the AP-loaded RSF nanoparticles ranged from 200 to 1000 nm, and the nanoparticles were spherically shaped, as seen by transmission electron microscopy. The drug loading and encapsulation efficiency were about 25.9% and 87.3%, respectively. Furthermore, the release time of AP-loaded RSF nanoparticles was about 3 days. The particle size and drug release behaviour could be adjusted by treating with glycol amine. The cytotoxicity studies demonstrated that the RSF nanoparticles showed negligible cytotoxicity to cells, and the anti-proliferative activity of AP-loaded RSF nanoparticles showed that the AP-loaded RSF nanoparticles can adhere to Hela cells and MDA-MB-231 cells easily. All these results imply that this biomacromolecule drug nanocarrier has great potential for chemotherapy in clinical applications.
穿心莲内酯(AP)是一种从[具体植物]中分离出的二萜类化合物,具有广泛的生物活性,包括抗炎、抗癌、保肝和降血脂作用。然而,其水溶性差和稳定性低导致生物利用度较低,这严重限制了其药理功能。在本研究中,报道了尝试使用再生丝素蛋白(RSF)作为药物载体来包封AP。通过一种简便且无污染的方法,在不使用任何有毒试剂的情况下制备了负载AP的RSF纳米颗粒。此外,特别关注了制剂的优化。最后,通过透射电子显微镜观察,负载AP的RSF纳米颗粒的尺寸范围为200至1000nm,且纳米颗粒呈球形。载药量和包封率分别约为25.9%和87.3%。此外,负载AP的RSF纳米颗粒的释放时间约为3天。通过用乙醇胺处理可以调节粒径和药物释放行为。细胞毒性研究表明,RSF纳米颗粒对细胞的细胞毒性可忽略不计,负载AP的RSF纳米颗粒的抗增殖活性表明其可以轻松粘附于Hela细胞和MDA-MB-231细胞。所有这些结果表明,这种生物大分子药物纳米载体在临床应用中的化疗方面具有巨大潜力。