Pharmaceutical Technology Department, National Research Centre, Dokki, Cairo, Egypt.
Pharmaceutical Technology Department, National Research Centre, Dokki, Cairo, Egypt.
J Pharm Sci. 2021 Jul;110(7):2677-2686. doi: 10.1016/j.xphs.2021.02.007. Epub 2021 Feb 16.
Coenzyme Q10 (CoQ10) acts as an antioxidant that protects the cells by preventing lipid peroxidation. Owing to its low solubility, CoQ10 has shown poor delivery properties and poor bioavailability. The aim of this study is to develop CoQ10 loaded cubosomes in order to enhance its oral delivery and hepatoprotective activity. Cubosomes are cubic nanostructured systems resulting from the colloidal dispersion of cubic liquid crystalline structure in water. CoQ10 loaded cubosomes were prepared using poloxamer 407 and glyceryl monooleate at three weight ratios (1:2.5, 1:5 and 1:7.5) and were further characterized. They were investigated for their hepatoprotective effect in thioacetamide (TAA) induced hepatotoxicity in Wistar rats. The developed CoQ10 cubosomes exhibited moderate to high entrapment efficiency percentages (44.69-75.96%), nanometric dimensions (132.4-223.2 nm), and negatively charged zeta potential values (<-21.3). In-vitro release profiles showed a sustained release of CoQ10 from the developed cubosomes up to 48 h. In-vivo study revealed an improved hepatoprotective effect of CoQ10 cubosomes via reducing liver enzymes, nitric oxide and malondialdehyde as well as elevating phosphoinositide 3-kinase, catalase and glutathione peroxidase, compared to plain drug. These results were in good agreement with histopathological investigations. Consequently, the developed cubosomes showed a potential effect in enhancing the hepatoprotective activity of CoQ10.
辅酶 Q10（CoQ10）作为一种抗氧化剂，通过防止脂质过氧化来保护细胞。由于其低溶解度，CoQ10 表现出较差的传递性能和较差的生物利用度。本研究旨在开发负载 CoQ10 的立方脂质体纳米囊泡，以提高其口服递送和肝保护活性。立方脂质体纳米囊泡是由立方液晶结构在水中胶体分散形成的立方纳米结构体系。使用泊洛沙姆 407 和甘油单油酸酯以三种重量比（1:2.5、1:5 和 1:7.5）制备负载 CoQ10 的立方脂质体纳米囊泡，并对其进行了进一步的特性研究。在 Wistar 大鼠中，研究了它们在硫代乙酰胺（TAA）诱导的肝毒性中的肝保护作用。所开发的 CoQ10 立方脂质体纳米囊泡表现出中等至高的包封效率百分比（44.69-75.96%）、纳米尺寸（132.4-223.2nm）和带负电荷的 Zeta 电位值（<-21.3mV）。体外释放曲线显示 CoQ10 从开发的立方脂质体纳米囊泡中持续释放长达 48 小时。体内研究表明，与普通药物相比，CoQ10 立方脂质体纳米囊泡通过降低肝酶、一氧化氮和丙二醛以及提高磷酸肌醇 3-激酶、过氧化氢酶和谷胱甘肽过氧化物酶，具有改善的 CoQ10 的肝保护作用。这些结果与组织病理学研究结果一致。因此，开发的立方脂质体纳米囊泡显示出增强 CoQ10 肝保护活性的潜力。
