Chen Li, Wei Junxia, An Mengying, Zhang Li, Lin Shiyu, Shu Gang, Yuan Zhixiang, Lin Juchun, Peng Guangneng, Liang Xiaoxia, Yin Lizi, Zhang Wei, Zhao Ling, Fu Hualin
Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan, 611130, China.
College of Pharmacy, Southwest Minzu University, Chengdu, Sichuan, 610225, China.
Colloids Surf B Biointerfaces. 2020 Nov;195:111221. doi: 10.1016/j.colsurfb.2020.111221. Epub 2020 Jun 25.
Mequindox (Meq) is a promising broad-spectrum antibacterial agent, but the clinical application of Meq has been hampered by its low oral bioavailability. Casein (Cas) can bind to a variety of poorly water-soluble drugs to improve their water solubility through a micellar solubilization mechanism. Here, a low-cost and convenient method was introduced to prepare mequindox-loaded casein nanoparticles (Meq-Cas). Meq-Cas was characterized by several methods including differential scanning calorimetry (DSC), X-ray diffraction (XRD), and fourier transform infrared (FTIR) to illuminate the mutual effect between the drug and carriers. Meq-Cas presented nearly spherical nanoparticles with smooth surfaces and its mean particle size was lower than untreated Cas. Meq-Cas showed a nearly complete release of Meq, which displayed a biphasic drug release pattern in both phosphate-buffered solution (PBS) and simulated gastric fluid (SGF). The relative oral bioavailability of Meq-Cas was found to be about 1.20 times higher than that of the animals treated with Meq suspension (control). These results suggest that Cas is a good candidate to load in Meq for pharmaceutical purposes.
乙酰甲喹（Meq）是一种很有前景的广谱抗菌剂，但其口服生物利用度较低，阻碍了其临床应用。酪蛋白（Cas）可与多种难溶性药物结合，通过胶束增溶机制提高其水溶性。在此，引入了一种低成本且简便的方法来制备载乙酰甲喹的酪蛋白纳米粒（Meq-Cas）。通过差示扫描量热法（DSC）、X射线衍射（XRD）和傅里叶变换红外光谱（FTIR）等多种方法对Meq-Cas进行表征，以阐明药物与载体之间的相互作用。Meq-Cas呈现出表面光滑的近球形纳米粒，其平均粒径低于未处理的Cas。Meq-Cas显示出Meq几乎完全释放，在磷酸盐缓冲溶液（PBS）和模拟胃液（SGF）中均呈现双相药物释放模式。发现Meq-Cas的相对口服生物利用度比用Meq悬浮液处理的动物（对照）高约1.20倍。这些结果表明，Cas是用于药物目的负载Meq的良好候选物。
