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在溶菌酶溶液中戊二醛交联壳聚糖纳米颗粒的体外酶消化率及其在肺部药物传递中的应用。

In Vitro Enzymatic Digestibility of Glutaraldehyde-Crosslinked Chitosan Nanoparticles in Lysozyme Solution and Their Applicability in Pulmonary Drug Delivery.

机构信息

Pharmacy Discipline, School of Clinical Sciences, Faculty of Health, Queensland University of Technology (QUT), Brisbane, QLD 4000, Australia.

Institute of Health and Biomedical Innovation, QUT, 60 Musk Avenue, Kelvin Grove, Brisbane, QLD 4059, Australia.

出版信息

Molecules. 2019 Apr 1;24(7):1271. doi: 10.3390/molecules24071271.

Abstract

Herein, the degradation of low molecular weight chitosan (CS), with 92% degree of deacetylation (DD), and its nanoparticles (NP) has been investigated in 0.2 mg/mL lysozyme solution at 37 °C. The CS nanoparticles were prepared using glutaraldehyde crosslinking of chitosan in a water-in-oil emulsion system. The morphological characterization of CS particles was carried out using scanning electron microscopy (SEM) and Transmission Electron Microscopy (TEM) techniques. Using attenuated total reflectance Fourier transform infrared (ATR-FTIR) and UV-VIS spectroscopy, the structural integrity of CS and its NPs in lysozyme solution were monitored. The CS powder showed characteristic FTIR bands around 1150 cm associated with the glycosidic bridges (C-O-C bonds) before and after lysozyme treatment for 10 weeks, which indicated no CS degradation. The glutaraldehyde crosslinked CS NPs showed very weak bands associated with the glycosidic bonds in lysozyme solution. Interestingly, the UV-VIS spectroscopic data showed some degradation of CS NPs in lysozyme solution. The results of this study indicate that CS with a high DD and its NPs crosslinked with glutaraldehyde were not degradable in lysozyme solution and thus unsuitable for pulmonary drug delivery. Further studies are warranted to understand the complete degradation of CS and its NPs to ensure their application in pulmonary drug delivery.

摘要

本文研究了在 37°C 的 0.2mg/mL 溶菌酶溶液中,具有 92%脱乙酰度(DD)的低分子量壳聚糖(CS)及其纳米颗粒(NP)的降解情况。CS 纳米颗粒是通过水包油乳液体系中的壳聚糖戊二醛交联制备的。使用扫描电子显微镜(SEM)和透射电子显微镜(TEM)技术对 CS 颗粒的形态特征进行了表征。使用衰减全反射傅里叶变换红外(ATR-FTIR)和紫外-可见光谱法监测 CS 及其 NPs 在溶菌酶溶液中的结构完整性。CS 粉末在溶菌酶处理前和处理后 10 周时,在 1150cm 左右表现出与糖苷键(C-O-C 键)相关的特征 FTIR 带,这表明 CS 没有降解。戊二醛交联的 CS NPs 在溶菌酶溶液中显示出与糖苷键相关的非常弱的带。有趣的是,紫外-可见光谱数据显示 CS NPs 在溶菌酶溶液中有一些降解。这项研究的结果表明,具有高 DD 的 CS 及其与戊二醛交联的 NPs 不能在溶菌酶溶液中降解,因此不适合用于肺部药物输送。需要进一步研究以了解 CS 及其 NPs 的完全降解情况,以确保其在肺部药物输送中的应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f593/6480642/ae582e6aba2d/molecules-24-01271-sch001.jpg

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