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首页> 外文期刊>Acta biomaterialia >Entirely S-protected chitosan: A promising mucoadhesive excipient for metronidazole vaginal tablets
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Entirely S-protected chitosan: A promising mucoadhesive excipient for metronidazole vaginal tablets

机译：完全是S保护的壳聚糖：用于甲硝唑阴道片的有希望的粘膜胶粘剂

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Graphical abstract Display Omitted Abstract Aim Synthesis and evaluation of an entirely S-protected chitosan as mucoadhesive excipient for vaginal drug delivery. Methods N-acetyl-cysteine was linked to 6-mercaptonicotinamide via disulphide exchange reaction. The obtained ligand, NAC-6-MNA, was subsequently attached to chitosan by carbodiimide mediated amide bond formation in two concentrations. The synthesized S-protected chitosan was chemically characterized and mucoadhesive properties and stability against oxidation were investigated. Moreover, metronidazole tablets comprising the S-protected chitosan were evaluated regarding water uptake capacity, disintegration behaviour, residence time on vaginal mucosa, release of the encapsulated drug and antimicrobial activity. Results S-protected chitosan displayed 160±19 (CS-MNA-160) and 320±38 (CS-MNA-320)μmol of ligand per gram of polymer. At pH 4.2, CS-MNA-160 and CS-MNA-320 showed 5.2-fold and 6.2-fold increase in mucus viscosity in comparison to unmodified chitosan (One-way ANOVA, p p Conclusions On the basis of the achieved results, entirely S-protected chitosan represents a promising excipient for the development of metronidazole vaginal tablets. Statement of Significance S-protected thiomers are polymers modified with thiol groups protected by aromatic ligands and characterized by strong mucoadhesive properties and high stability against oxidation. Up to date, the entirely S-protection of thiol groups was achieved via the synthesis of the ligand 2-((2-amino-2-carboxyethyl)disulfanyl)nicotinic acid) which can be directly bound to the backbone of polymers bearing carboxylic moieties as pectin. However, this ligand is not suitable for positively charged polymers due to the negative charge. In this paper, the synthesis of a suitable ligand for the entirely S-protection of positively charged polymers is presented. The first entirely S-protected chitosan was synthesized, characterized and its mucoadhesive properties were assessed. Moreover, metronidazole tablets comprising the entirely S-protected chitosan were developed and evaluated as vaginal drug delivery system.
机译：图形摘要显示省略了摘要摘要旨在对含阴道药物递送的粘膜粘附赋形剂的完全受保护的壳聚糖。方法通过二硫化物交换反应将N-乙酰基半胱氨酸与6-巯基辛酰胺连接。随后通过碳二酰亚胺介导的氨基酰胺键在两种浓度下与壳聚糖连接到壳聚糖的配体NaC-6-MNA。合成的S保护的壳聚糖化学表征，研究了粘膜粘附性和稳定性的氧化稳定性。此外，在阴影能力，崩解行为，阴道粘膜上的停留时间，释放包封的药物和抗微生物活性，评估包含S保护的壳聚糖的甲硝唑片剂。结果S保护壳聚糖显示160±19（CS-MNA-160）和320±38（CS-MNA-320）μmol/克聚合物。在pH4.2，与未修饰的壳聚糖（单向ANOVA，PP结论在达到的结果的基础上，CS-MNA-160和CS-MNA-320显示出5.2倍和6.2倍的粘液粘度增加6.2倍，粘液粘度为6.2倍。 - 保护的壳聚糖代表了甲硝唑阴道片的发育的有希望的赋形剂。显着性S保护的硫代的硫聚物是用芳族配体保护的硫醇基改性的聚合物，其特征在于强烈的粘液性能和抗氧化稳定性。最新，完全是最新的通过合成配体2 - （（2-氨基-2-羧基）二磺酰基）烟酸的合成来实现硫醇基团的保护，该烟酸可以直接与含有羧基部分的聚合物的骨架结合。然而，由于负电荷，该配体不适用于带正电荷的聚合物。本文介绍了适合于完全带正电荷聚合物的合适配体的合成。合成了第一个完全保护的壳聚糖，其特征在一起，并评估其粘膜粘附性质。此外，制定了包含全面保护的壳聚糖的甲硝唑片，并评估为阴道药物递送系统。

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