一种新型槲皮素包封葡萄糖修饰的脂质体及其脑靶向抗氧化神经保护作用。

A Novel Quercetin Encapsulated Glucose Modified Liposome and Its Brain-Target Antioxidative Neuroprotection Effects.

机构信息

Institute of Agro-Products Processing Science and Technology, Institute of Food Nutrition and Health, Sichuan Academy of Agricultural Sciences, Chengdu 610066, China.

Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.

出版信息

Molecules. 2024 Jan 26;29(3):607. doi: 10.3390/molecules29030607.

Neurodegenerative diseases (NDDs) are mainly induced by oxidative stress which produces excessive reactive oxygen species (ROS). Quercetin (QU) is a potent antioxidant with some effects on NDDs. This study prepared and characterized a novel glucose-modified QU liposome (QU-Glu-Lip), aiming not only to overcome QU's poor water solubility and bioavailability but also to deliver more QU to brain tissue to enhance its neuroprotective effect. QU-Glu-Lip possessed encapsulation efficiency (EE) of 89.9%, homogenous particle sizes (116-124 nm), small PDI value (<0.3), zeta value -1.363 ± 0.437 mV, proper pH and salt stability, and proper cytotoxicity. The glucose-modified liposome penetrated the blood-brain barrier (BBB) mediated via the glucose transporter 1 (GLUT1) and was taken by neuronal cells more efficiently than liposome without glucose, according to bEnd.3 and PC12 cell tests. QU-Glu-Lip attenuated HO-induced oxidative damage to PC12 with higher cell viability (88.42%) and lower intracellular ROS compared to that of QU. QU-Glu-Lip had higher brain target ability and delivered more QU to neuronal cells, effectively exerting the antioxidative neuroprotection effect. There is potential for the QU-Glu-Lip application for more effective treatment of NDDs.

神经退行性疾病（NDDs）主要由氧化应激引起，氧化应激会产生过多的活性氧（ROS）。槲皮素（QU）是一种有效的抗氧化剂，对 NDDs 有一定的作用。本研究制备并表征了一种新型葡萄糖修饰的 QU 脂质体（QU-Glu-Lip），旨在克服 QU 较差的水溶性和生物利用度，并将更多的 QU 递送到脑组织，以增强其神经保护作用。QU-Glu-Lip 的包封效率（EE）为 89.9%，粒径均匀（116-124nm），PDI 值小（<0.3），zeta 值为-1.363±0.437mV，pH 值和盐度合适，细胞毒性合适。与没有葡萄糖的脂质体相比，葡萄糖修饰的脂质体通过葡萄糖转运蛋白 1（GLUT1）介导穿透血脑屏障（BBB），并更有效地被神经元细胞摄取。根据 bEnd.3 和 PC12 细胞试验，QU-Glu-Lip 减轻了 HO 诱导的 PC12 氧化损伤，细胞活力（88.42%）更高，细胞内 ROS 更低。QU-Glu-Lip 具有更高的脑靶向能力，并向神经元细胞输送更多的 QU，有效地发挥抗氧化神经保护作用。QU-Glu-Lip 有望更有效地治疗 NDDs。