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具有抗菌抗氧化活性的百里香酚-壳聚糖水凝胶用于口腔局部给药的研发与评价

Development and evaluation of thymol-chitosan hydrogels with antimicrobial-antioxidant activity for oral local delivery.

作者信息

Alvarez Echazú María Inés, Olivetti Christian Ezequiel, Anesini Claudia, Perez Claudio Javier, Alvarez Gisela Solange, Desimone Martin Federico

机构信息

Universidad de Buenos Aires, Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET), Instituto de Química y Metabolismo del Fármaco (IQUIMEFA), Facultad de Farmacia y Bioquímica, Junín 956, Piso 3° (1113), Buenos Aires, Argentina.

Instituto de Investigaciones en Ciencia y Tecnología de Materiales (INTEMA), Grupo Ciencia y Tecnología de Polímeros, Universidad Nacional de Mar del Plata, Juan B. Justo 4302, (7600) Mar del Plata, Argentina.

出版信息

Mater Sci Eng C Mater Biol Appl. 2017 Dec 1;81:588-596. doi: 10.1016/j.msec.2017.08.059. Epub 2017 Aug 15.

Abstract

Nowadays, the research of innovative drug delivery devices is focused on the design of multiple drug delivery systems, the prevention of drug side effects and the reduction of dosing intervals. Particularly, new mucosal delivery systems for antimicrobials, antioxidants and anti-inflammatory drugs has a growing development, regards to the avoidance of side effects, easy administration and a suitable drug concentration in the mucosa. In this work, chitosan hydrogels are evaluated as a biodegradable scaffold and as a bioactive agent carrier of an antioxidant-antimicrobial compound called thymol. Throughout the study, swelling behavior, viscoelastic properties and thermal analysis are highlighted to present its advantages for a biomedical application. Furthermore, the in vitro results obtained indicate that thymol-chitosan hydrogels are biocompatible when exposed to [3T3] fibroblasts, exhibit antimicrobial activity against Staphylococcus aureus and Streptococcus mutans for 72h and antioxidant activity for 24h. These are desirable properties for a mucosal delivery system for an antimicrobial-antioxidant dual therapy for periodontal disease.

摘要

如今,创新药物递送装置的研究集中在多药物递送系统的设计、药物副作用的预防以及给药间隔的缩短上。特别是,用于抗菌、抗氧化和抗炎药物的新型粘膜递送系统发展迅速,这是因为其具有避免副作用、给药方便以及在粘膜中药物浓度适宜等优点。在这项工作中,壳聚糖水凝胶被评估为一种可生物降解的支架以及一种名为百里香酚的抗氧化抗菌化合物的生物活性剂载体。在整个研究过程中,突出了其溶胀行为、粘弹性特性和热分析,以展示其在生物医学应用中的优势。此外,获得的体外结果表明,百里香酚 - 壳聚糖水凝胶在暴露于[3T3]成纤维细胞时具有生物相容性,对金黄色葡萄球菌和变形链球菌具有72小时的抗菌活性以及24小时的抗氧化活性。这些是用于牙周病抗菌 - 抗氧化双重治疗的粘膜递送系统的理想特性。

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