Biotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, 91775-1365, Iran; Nanotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran; Department of Pharmaceutical Biotechnology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, 91775-1365, Iran.
Nanotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran; Department of Pharmaceutical Nanotechnology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, 91775-1365, Iran.
Colloids Surf B Biointerfaces. 2020 Oct;194:111203. doi: 10.1016/j.colsurfb.2020.111203. Epub 2020 Jun 17.
In this study using phospholipids with high transition temperature and taking advantage of PEGylation, we designed liposomal formulation targeted with folic acid (FA) to improve the stability of liposomes with high penetration efficiency at the same time. The results of characterization demonstrated that liposomal formulations are in range of 150-210 nm size with negative surface charge. The results of cell uptake indicated that FA conjugation resulted in the more uptake of insulin. However, the results of transepithelial electrical resistance (TEER) showed no statistical differences among the formulations. The results of biodistribution also demonstrated that PEGylated liposome targeted with FA had more residence time in stomach and intestine along with higher amounts in blood and liver. The anti-diabetic effects of formulation in vivo indicated the efficacy of PEGylated liposome targeted with FA had promising results in decreasing blood glucose and increasing insulin levels. The results of this study indicated that using phospholipids with high Tm along with PEGylation and using targeting ligand could improve efficiency of oral delivery of liposomes which merit further investigation.
在这项使用具有高相变温度的磷脂并利用聚乙二醇化的研究中，我们设计了靶向叶酸（FA）的脂质体配方，以提高具有高穿透效率的脂质体的稳定性。表征结果表明，脂质体配方的粒径在 150-210nm 之间，带负电荷。细胞摄取结果表明，FA 缀合导致胰岛素摄取增加。然而，跨上皮电阻（TEER）的结果表明，各配方之间没有统计学差异。体内分布结果也表明，靶向 FA 的聚乙二醇化脂质体在胃和肠道中的停留时间更长，血液和肝脏中的含量更高。体内抗糖尿病作用表明，靶向 FA 的聚乙二醇化脂质体具有降低血糖和提高胰岛素水平的良好效果。本研究结果表明，使用具有高热力学相变温度的磷脂，结合聚乙二醇化和使用靶向配体，可以提高脂质体口服递送的效率，值得进一步研究。
