Molecular Physiology Division, Faculty of Science, Beni-Suef University, Salah Salem St., 62511 Beni-Suef, Egypt.
Materials Science and Nanotechnology Department, Faculty of Postgraduate Studies for Advanced Sciences (PSAS), Beni-Suef University, Egypt.
Int J Biol Macromol. 2020 Jul 1;154:1496-1504. doi: 10.1016/j.ijbiomac.2019.11.031. Epub 2019 Nov 20.
Polydatin (PD) has many pharmacological activities; however, its bioavailability is still a critical cornerstone issue. The present investigation aimed to develop a novel oral formula of polydatin-loaded chitosan nanoparticles (PD-CSNPs) to improve PD therapeutic potential against type 2 diabetes. The interaction mechanism between PD and CSNPs was studied via Monte Carlo and molecular dynamics simulations. The formula was prepared and characterized by FTIR, XRD, TEM, and dynamic light scattering. The release profile of PD was studied in vitro, as well as the cytotoxicity effect versus Vero cell line and antidiabetic activity in type 2 diabetic rats were investigated. The practical results verified the formation of PD-CSNPs with entrapment efficiency of about 96.74 ± 0.39%, size average 144.25 ± 3.37 nm, and the prolonged release pattern was less than 20% after 12 hrs. The cytotoxicity study confirmed the safety of the formula at low and high doses. Moreover, the in vivo study revealed that PD-CSNPs exhibited highly significant antidiabetic efficacy in diabetic rats compared to free PD. To conclude, the current investigation proved that CSNPs are promising nanocarriers for nontoxic and effective PD delivery against type 2 diabetes.
虎杖苷（PD）具有多种药理活性，但生物利用度仍是一个关键问题。本研究旨在开发一种新的载虎杖苷壳聚糖纳米粒（PD-CSNPs）口服配方，以提高 PD 治疗 2 型糖尿病的潜力。通过蒙特卡罗和分子动力学模拟研究了 PD 与 CSNPs 之间的相互作用机制。通过傅里叶变换红外光谱（FTIR）、X 射线衍射（XRD）、透射电子显微镜（TEM）和动态光散射对配方进行了制备和表征。研究了 PD 的体外释放特性，以及对 Vero 细胞系的细胞毒性作用和对 2 型糖尿病大鼠的抗糖尿病活性。实际结果验证了 PD-CSNPs 的形成，其包封效率约为 96.74±0.39%，平均粒径为 144.25±3.37nm，12 小时后释放模式延长，释放量小于 20%。细胞毒性研究证实了该配方在低剂量和高剂量下的安全性。此外，体内研究表明，与游离 PD 相比，PD-CSNPs 在糖尿病大鼠中表现出显著的抗糖尿病功效。总之，本研究证明 CSNPs 是一种有前途的无毒有效递送 PD 治疗 2 型糖尿病的纳米载体。
