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基于聚阴离子聚合物的冻干基质用于口腔和阴道腔道中氯己定的局部释放。

Freeze-Dried Matrices Based on Polyanion Polymers for Chlorhexidine Local Release in the Buccal and Vaginal Cavities.

机构信息

Department of Pharmacy and Biotechnology, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy.

Department of Pharmacy and Biotechnology, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy.

出版信息

J Pharm Sci. 2019 Jul;108(7):2447-2457. doi: 10.1016/j.xphs.2019.02.026. Epub 2019 Mar 7.

Abstract

Chlorhexidine (CLX) is a wide spectrum cationic antimicrobial used for prevention and treatment of infections of buccal and vaginal cavities. To increase the residence time of CLX-based formulations at the application site and consequently reduce the daily dose frequency, new formulations composed of mucoadhesive polymers should be designed. The objective of this work was the development of matrices based on polyanionic polymers, such as sodium alginate, carboxymethylcellulose, xanthan gum and sodium hyaluronate, aimed to prolong the local release of CLX into the buccal or vaginal cavity. Matrices were prepared by freeze-drying and comply with 2 different preparative methods and characterized in terms of resistance to compression, water uptake ability, mucoadhesion, in vitro drug release behavior and antimicrobial activity toward representative pathogens of buccal and vaginal cavities. Results showed that the selection of suitable polymers associated to the adequate preparative method allowed to modulate matrix ability to hydrate, adhere to the mucosa and release the drug as well as to exert antimicrobial activity. In particular, matrix based on sodium hyaluronate was found to be the best performing formulation and could represent a versatile system for local release of CLX with potential application in both buccal and vaginal cavities.

摘要

洗必泰(CLX)是一种广谱阳离子抗菌药物,用于预防和治疗口腔和阴道腔的感染。为了增加基于 CLX 的制剂在应用部位的停留时间,从而减少每日剂量频率,应设计由具有粘膜粘附性的聚合物组成的新制剂。这项工作的目的是开发基于聚阴离子聚合物(如海藻酸钠、羧甲基纤维素、黄原胶和透明质酸钠)的基质,旨在延长 CLX 向口腔或阴道腔的局部释放。基质通过冷冻干燥制备,并符合 2 种不同的制备方法,其特性为抗压性、吸水性、粘膜粘附性、体外药物释放行为以及对口腔和阴道腔代表性病原体的抗菌活性。结果表明,选择合适的聚合物并结合适当的制备方法可以调节基质的水化、粘附和释放药物以及发挥抗菌活性的能力。特别是,基于透明质酸钠的基质被发现是性能最佳的制剂,它可以作为 CLX 局部释放的多功能系统,具有在口腔和阴道腔中应用的潜力。

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