Novel polydatin-loaded chitosan nanoparticles for safe and efficient type 2 diabetes therapy: In silico, in vitro and in vivo approaches
Novel polydatin-loaded chitosan nanoparticles for safe and efficient type 2 diabetes therapy: In silico, in vitro and in vivo approaches
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DOI：
10.1016/j.ijbiomac.2019.11.031
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发表时间：
2020-07-01
影响因子：
8.2
通讯作者：
Taha, Mohamed
中科院分区：
文献类型：
--
作者：
Abdel-Moneim, Adel;El-Shahawy, Ahmed;Taha, Mohamed
白藜芦醇苷（PD）具有多种药理活性，但其生物利用度仍是一个关键的基础问题。本研究旨在开发一种新的口服制剂--载虎杖苷的壳聚糖纳米粒（PD-CSNPs），以提高PD治疗2型糖尿病的潜力。通过Monte Carlo和分子动力学模拟研究了PD与CSNPs的相互作用机理。采用FTIR、XRD、TEM、动态光散射等手段对该复合材料进行了表征。研究了PD的体外释药特性、对Vero细胞的细胞毒性和对2型糖尿病大鼠的降糖活性。实际结果验证了PD-CSNPs的形成，其包封率约为96.74 ± 0.39%，平均粒径为144.25 ± 3.37 nm，并且在12小时后的延长释放模式小于20%。细胞毒性研究证实了低剂量和高剂量配方的安全性。此外，体内研究表明，PD-CSNP在糖尿病大鼠中表现出与游离PD相比非常显著的抗糖尿病功效。总之，目前的研究证明，CSNPs是一种有前途的纳米载体，可用于无毒和有效的PD治疗2型糖尿病。(C)2019 Elsevier B. V.版权所有。
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. (C) 2019 Elsevier B.V. All rights reserved.