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羧甲基淀粉:碘抗感染复合物:扩展的 v 螺旋结构与增强的黏膜黏附性。

Carboxymethyl-starch: iodine anti-infective complexes: expanded v-helix and increased mucoadhesion.

作者信息

Tajer Salma, Labelle Marc-André, Ispas-Szabo Pompilia, Mateescu Mircea Alexandru

机构信息

Department of Chemistry, Faculty of Science, Proteo Centre, Université du Québec à Montréal, POB 8888, Branch A, Montreal (QC), H3C 3P8, Canada.

Department of Chemistry, Faculty of Science, Proteo Centre, Université du Québec à Montréal, POB 8888, Branch A, Montreal (QC), H3C 3P8, Canada.

出版信息

Int J Pharm. 2025 Sep 15;682:125911. doi: 10.1016/j.ijpharm.2025.125911. Epub 2025 Jun 27.

DOI:10.1016/j.ijpharm.2025.125911
PMID:40582525
Abstract

BACKGROUND

There is a major need of novel approaches to limit contamination with respiratory viruses such as SARS-CoV-2 (Covid 19) and inluenza.

RATIONALE

Since the viral transmission is by aerosols, the oral and nasopharyngeal decontamination seems of relevance to prevent virus spreading. The hypothesis was that CMS, grafted with polar carboxylic groups, may present expanded V-helices, helping to load higher amounts of iodine.

METHODOLOGY

Carboxymethylstarch (CMS) having a degree of substitution between 0.15-0.30, microspheres of CMS cross-linked with Sodium TriMetaPhosphate (STMP), and high amylose starch cross-linked (CL) with epichlorohydrin HAS-CL(5,10) were proposed as matrices for iodine inclusion complexes for application as anti-infective agents. The sublimated iodine vapor was spontaneously included in the CMS matrices with no interventions during loading. This was found for CMS only and did not occur with non-derivatized starch. The morphology and the corresponding iodine-loaded formulations have been characterized by Fourier transform infrared spectroscopy, X-ray diffraction and scanning electron microscopy.

RESULTS

X-ray diffraction patterns of CMS, showed the peaks characteristic of B-type helices vanished whereas peaks (at 20° and 22°) characteristic of the V-type (simple helix) have been strengthened. Furthermore, by hydrolysis of CMS matrix with alpha-amylase, the released iodine would act against infective agents (i.e. respiratory viruses). The iodine complexation induced some structural modifications on the CMS network. CMS:I presented an enhanced mucoadhesion, a markedly increased sprayability, and a higher susceptibility at amylolysis with alpha-amylase, when compared to unloaded CMS.

CONCLUSIONS

The novel CMS:I complexes appear as potential virucidal agents (supported by a recent investigation).

摘要

背景

迫切需要新方法来限制呼吸道病毒如严重急性呼吸综合征冠状病毒2(SARS-CoV-2,新冠病毒19)和流感病毒的污染。

原理

由于病毒通过气溶胶传播,口腔和鼻咽去污对于预防病毒传播似乎具有重要意义。假设是,接枝有极性羧基的羧甲基淀粉(CMS)可能呈现扩展的V型螺旋,有助于负载更多量的碘。

方法

提出取代度在0.15 - 0.30之间的羧甲基淀粉(CMS)、与三聚磷酸钠(STMP)交联的CMS微球以及与环氧氯丙烷交联的高直链淀粉(HAS-CL(5,10))作为碘包合物的基质,用作抗感染剂。升华的碘蒸气在负载过程中无需干预即可自发地包含在CMS基质中。仅在CMS中发现了这种情况,未衍生化的淀粉则不会发生。通过傅里叶变换红外光谱、X射线衍射和扫描电子显微镜对形态以及相应的载碘制剂进行了表征。

结果

CMS的X射线衍射图谱显示,B型螺旋的特征峰消失,而V型(简单螺旋)的特征峰(在20°和22°处)增强。此外,通过用α-淀粉酶水解CMS基质,释放的碘将对感染因子(即呼吸道病毒)起作用。碘络合对CMS网络诱导了一些结构修饰。与未负载碘的CMS相比,CMS:I表现出增强的粘膜粘附性、显著提高的喷雾性以及对α-淀粉酶淀粉分解的更高敏感性。

结论

新型CMS:I络合物似乎是潜在的杀病毒剂(最近的一项研究提供了支持)。

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