Yadav Yogesh Chand, Pattnaik Satyanarayan
Department of Pharmacology, Faculty of Pharmacy, UP University of Medical Sciences, Saifai, Etawah, India.
Talla Padmavathi College of Pharmacy, Warangal, India.
Drug Dev Ind Pharm. 2023 Feb;49(2):240-247. doi: 10.1080/03639045.2023.2201625. Epub 2023 Apr 19.
The purpose of the study is to assess the bioavailability and neuroprotective effect of hesperetin (Hesp)-loaded nanofibers.
Electrospinning was used to create and characterize polyvinyl pyrrolidone-based Hesp-loaded nanofibers. To evaluate the produced nanofibers, preclinical studies were conducted. The study involved five groups of Wistar rats, and the treatments were administered as follows. Group 1 (control) was given regular saline for 14 d. On the 14th day, Group 2 was given scopolamine. Group 3 was given donepezil for 14 d and then scopolamine on the 14th. Group 4 was given Hesp for 14 d and then scopolamine on the 14th. Group 5 was given Hesp-loaded nanofibers for 14 d, followed by scopolamine on the 14th. On the 14th day, rats' memory was tested using Cook's pole climbing apparatus and the Morris water maze (MWM). On the 15th day, rats from each group were slaughtered, brain tissues were separated, and biochemical and histological analyses were performed. In addition, dissolution experiments and pharmacokinetic studies were carried out.
When compared to the control group, scopolamine-treated rats had considerably longer escape latency times, as well as increased acetylcholinesterase (AChE) activity, lipid peroxidation, degeneration, and inflammation in the hippocampus. These parameters were greatly recovered by donepezil and Hesp-loaded nanofibers that had been pretreated. Because of the greatly improved bioavailability of Hesp, the Hesp-loaded nanofibers significantly protected rats from scopolamine-induced amnesia.
Hesp-loaded nanofibers have an excellent neuroprotective effect against scopolamine-induced amnesia due to enhanced bioavailability.
本研究旨在评估载有橙皮素（Hesp）的纳米纤维的生物利用度和神经保护作用。
采用静电纺丝法制备并表征基于聚乙烯吡咯烷酮的载有Hesp的纳米纤维。为评估所制备的纳米纤维，进行了临床前研究。该研究涉及五组Wistar大鼠，治疗给药方式如下。第1组（对照组）给予常规生理盐水，持续14天。在第14天，第2组给予东莨菪碱。第3组给予多奈哌齐14天，然后在第14天给予东莨菪碱。第4组给予Hesp 14天，然后在第14天给予东莨菪碱。第5组给予载有Hesp的纳米纤维14天，随后在第14天给予东莨菪碱。在第14天，使用库克爬杆装置和莫里斯水迷宫（MWM）测试大鼠的记忆力。在第15天，宰杀每组大鼠，分离脑组织，并进行生化和组织学分析。此外，还进行了溶出实验和药代动力学研究。
与对照组相比，经东莨菪碱处理的大鼠逃避潜伏期明显更长，海马体中的乙酰胆碱酯酶（AChE）活性、脂质过氧化、变性和炎症也有所增加。这些参数通过预处理的多奈哌齐和载有Hesp的纳米纤维得到了显著恢复。由于Hesp的生物利用度大大提高，载有Hesp的纳米纤维显著保护大鼠免受东莨菪碱诱导的失忆。
载有Hesp的纳米纤维由于生物利用度提高，对东莨菪碱诱导的失忆具有优异的神经保护作用。
