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新型生物相容性聚(丙烯酰胺)接枝葡聚糖水凝胶:合成、表征及生物医学应用。

Novel biocompatible poly(acrylamide)-grafted-dextran hydrogels: Synthesis, characterization and biomedical applications.

机构信息

Department of Pharmaceutics, BLDEA's SSM College of Pharmacy and Research Centre, Vijayapur 586 103, Karnataka, India.

School of Chemical and Biomolecular Engineering, The University of Sydney, Sydney, NSW 2006, Australia.

出版信息

J Microbiol Methods. 2019 Apr;159:200-210. doi: 10.1016/j.mimet.2019.03.009. Epub 2019 Mar 12.

DOI:10.1016/j.mimet.2019.03.009
PMID:30877016
Abstract

An electro-responsive PAAm-g-Dxt copolymer was synthesized and characterized by HNMR & FTIR spectroscopy, neutralization equivalent, elemental and thermogravimetric analysis to ascertain the grafting reaction. Further, we developed an electro-responsive transdermal drug delivery system (ETDS) utilizing PAAm-g-Dxt copolymer for rivastigmine tartarate delivery through skin. The ETDS were developed using drug-loaded PAAm-g-Dxt hydrogel as the reservoir, and cross-linked dextran-poly(vinyl alcohol) blend films as rate controlling membranes (RCM). In the absence of electrical stimuli, a small amount of drug was permeated from the ETDS, while in the presence of electrical stimuli, the drug permeability was increased. On application of electric stimulus, the flux was increased by 1.6 fold; drug permeability was enhanced when the strength of applied electric current was raised to 8 mA from 2 mA. The drug permeability characteristics studied under "on-off" stimuli suggested that there was faster drug permeation when electrical stimuli was 'on' and it decreased when electrical stimuli was 'off.' The histopathology study confirmed the altered skin structural integrity after application of electrical stimuli. Hence, the PAAm-g-Dxt based ETDS are useful for transdermal drug delivery triggered by an electric stimulus to deliver on-demand release of drug into systemic circulation.

摘要

一种电响应性 PAAm-g-Dxt 共聚物通过 HNMR 和 FTIR 光谱、中和当量、元素分析和热重分析进行了合成和表征,以确定接枝反应。此外,我们利用 PAAm-g-Dxt 共聚物开发了一种电响应经皮药物传递系统 (ETDS),用于通过皮肤输送酒石酸瑞伐他汀。ETDS 是使用载药的 PAAm-g-Dxt 水凝胶作为储库,交联的葡聚糖-聚乙烯醇共混膜作为控释膜 (RCM) 开发的。在没有电刺激的情况下,少量药物从 ETDS 中渗透出来,而在有电刺激的情况下,药物的渗透性增加。施加电刺激时,通量增加了 1.6 倍;当施加的电流强度从 2mA 增加到 8mA 时,药物渗透性增强。在“开-关”刺激下研究的药物渗透性特征表明,当电刺激“开”时,药物渗透更快,当电刺激“关”时,药物渗透减少。组织病理学研究证实,施加电刺激后皮肤结构完整性发生改变。因此,基于 PAAm-g-Dxt 的 ETDS 可用于电刺激触发的经皮药物传递,以按需将药物递送到体循环中。

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