Complex liposomes were assembled with 1,2-distearoyl-sn-glycero-3-phosphocholine, dihexadecyl phosphate (DHDP), cholesterol and 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphate (PA) to act as drug carriers for resveratrol (RES) and epigallocatechin gallate (EGCG). The liposomes were modified with leptin (Lep) on the surface to cross the blood-brain barrier (BBB) and to rescue degenerated dopaminergic neurons. The activity of RES and EGCG against neurotoxicity was investigated using an in vitro neurodegenerative model established by SH-SY5Y cells with an insult of 1-methyl-4-phenylpyridinium (MPP⁺). The results indicated that increasing the mole percentage of DHDP and PA increased the particle size and absolute zeta potential value, and improved the entrapment efficiency of RES and EGCG; however, this increase reduced the release rate of RES and EGCG and the grafting efficiency of Lep. The ability of Lep/RES-EGCG-PA-liposomes to cross the BBB was found to be higher than that of non-modified liposomes. Further, the addition of PA and Lep into liposomes enhanced cell viability and target efficiency. The immunofluorescence results demonstrated that the conjugation of Lep with liposomes enabled the docking of HBMECs and SH-SY5Y cells via Lep receptor, and enhanced their ability to permeate the BBB and cellular uptake. Immunofluorescence and western blot analysis also revealed that RES and EGCG encapsulated into liposomes could be a neural defensive strategy by reducing the apoptosis promotor protein Bcl-2 associated X protein and α-synuclein, and enhancement in the apoptosis inhibitor protein B cell lymphoma 2, tyrosine hydroxylase, and the dopamine transporter. Hence, Lep-PA-liposomes can be an excellent choice of potential delivery system for PD treatment.

复合脂质体与1,2-二硬脂酰基-sn-甘油-3-磷酸胆碱，磷酸二十六烷基酯（DHDP），胆固醇和1-棕榈酰基-2-油酰基-sn-甘油-3-磷酸酯（PA）组装在一起用于白藜芦醇（RES）和表没食子儿茶素没食子酸酯（EGCG）。脂质体在表面上用瘦素（Lep）修饰，可以穿过血脑屏障（BBB）并挽救退化的多巴胺能神经元。使用由SH-SY5Y细胞建立的体外神经退行性模型，对1-甲基-4-苯基吡啶鎓（MPP ⁺）。结果表明，增加DHDP和PA的摩尔百分数可提高粒径和绝对ζ电位值，并提高RES和EGCG的包封率。但是，这种增加降低了RES和EGCG的释放速率以及Lep的嫁接效率。发现Lep / RES-EGCG-PA-脂质体穿过BBB的能力高于未修饰的脂质体。此外，将PA和Lep添加到脂质体中增强了细胞活力和靶效率。免疫荧光结果表明，Lep与脂质体的缀合使HBMECs和SH-SY5Y细胞通过Lep受体对接，增强了它们渗透BBB和细胞摄取的能力。免疫荧光和蛋白质印迹分析还表明，封装在脂质体中的RES和EGCG可通过减少凋亡促进蛋白Bcl-2相关的X蛋白和α-突触核蛋白并增强凋亡抑制剂蛋白B细胞淋巴瘤2，酪氨酸来作为神经防御策略。羟化酶和多巴胺转运蛋白。因此，Lep-PA-脂质体可以成为用于PD治疗的潜在递送系统的极佳选择。