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壳聚糖纳米薄膜和静电纺丝纳米纤维用于阿尔茨海默病的快速药物释放治疗:体外和体内评价。

Chitosan nanofilm and electrospun nanofiber for quick drug release in the treatment of Alzheimer's disease: In vitro and in vivo evaluation.

机构信息

Department of Chemistry, School of Advanced Sciences, VIT University, Vellore 632 014, Tamilnadu, India.

Department of Chemistry, School of Advanced Sciences, VIT University, Vellore 632 014, Tamilnadu, India.

出版信息

Int J Biol Macromol. 2017 Dec;105(Pt 1):131-142. doi: 10.1016/j.ijbiomac.2017.07.021. Epub 2017 Jul 8.

DOI:10.1016/j.ijbiomac.2017.07.021
PMID:28698078
Abstract

Chitosan micro sized ODF (CBF), chitosan nano sized ODF (CNF) and chitosan nanofiber (CNfib) were prepared to release the donepezil drug quickly for Alzheimer's disease. CNF and CNfib were prepared from ionic gelation technique and electro-spinning process which were further examined under in vitro and in vivo animal model studies. Good thermal stability of CNfib (450°C) when compared to CBF (325°C) and CNF (305°C). The particle size was below 150nm in diameter for CNfib and 250nm in diameter for CNF4 from TEM technique. In vitro antimicrobial activities for ODF and nanofibers were conducted by well diffusion method against Gram +ve and Gram -ve bacteria after 24h of incubation. From the in vitro release profile, the CNfib was competently showed rapid release of drug up to 97% than the thin film of CBF2 and CNF4 respectively in the initial period of 10min. In vivo animal model studies demonstrated that the drug reached the maximum concentration within 3.5h for chitosan nanofiber and nanofilm (CNF4). The chitosan nanofiber has given significantly faster absorption rate [1860.5ng/ml of AUC] and the mean total area under curve was 161.71% on contrasted with chitosan nanofilm (CNF4).

摘要

壳聚糖微 ODF(CBF)、壳聚糖纳米 ODF(CNF)和壳聚糖纳米纤维(CNfib)被制备用于快速释放多奈哌齐药物治疗阿尔茨海默病。CNF 和 CNfib 是通过离子凝胶技术和静电纺丝工艺制备的,进一步在体外和体内动物模型研究中进行了研究。与 CBF(325°C)和 CNF(305°C)相比,CNfib 具有良好的热稳定性(450°C)。TEM 技术显示,CNfib 的粒径小于 150nm,CNF4 的粒径为 250nm。ODF 和纳米纤维的体外抗菌活性通过抑菌圈法在孵育 24 小时后对革兰氏阳性菌和革兰氏阴性菌进行了检测。从体外释放曲线可以看出,在最初的 10 分钟内,CNfib 能够迅速释放药物,达到 97%,而 CBF2 和 CNF4 的薄膜分别为 97%和 97%。体内动物模型研究表明,壳聚糖纳米纤维在 3.5 小时内达到药物的最大浓度,而壳聚糖纳米纤维(CNF4)的 AUC 为 1860.5ng/ml,平均总曲线下面积为 161.71%。与壳聚糖纳米纤维(CNF4)相比,壳聚糖纳米纤维具有更快的吸收速度。

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