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含泊洛沙姆 407、聚乙烯醇和聚乙烯吡咯烷酮的粘膜粘附膜技术发展用于口腔甲硝唑传递。

Technological development of mucoadhesive film containing poloxamer 407, polyvinyl alcohol and polyvinylpyrrolidone for buccal metronidazole delivery.

机构信息

Laboratory of Research & Development of Drug Delivery Systems, Postgraduate Program in Pharmaceutical Sciences, Department of Pharmacy, State University of Maringa, Avenida Colombo, nº 5790, 87020-900, Maringa, Brazil.

出版信息

Ther Deliv. 2020 Jul;11(7):431-446. doi: 10.4155/tde-2020-0031. Epub 2020 Jul 5.

Abstract

This work aimed to develop a mucoadhesive film composed of a triblock copolymer (poloxamer 407), polyvinyl alcohol and polyvinylpyrrolidone for buccal modified delivery of metronidazole. Three film formulations containing different polymer amounts were prepared by solvent casting. They were characterized as physicochemical, mechanical and mucoadhesive properties, and metronidazole release profiles. Films displayed physicochemical, mechanical and mucoadhesive characteristics dependent of polymeric composition and drug presence. They could rapidly swell and promote the fast drug release (80% in 20 min) that was governed by Fickian diffusion. The films showed total disintegration in less than 90 s and total drug release in 30 min. Therefore, the formulations represent a promising alternative for modifying of buccal metronidazole delivery for pharmaceutical applications.

摘要

本工作旨在开发一种由三嵌段共聚物(泊洛沙姆 407)、聚乙烯醇和聚乙烯吡咯烷酮组成的粘膜粘附性薄膜,用于经口腔修饰传递甲硝唑。通过溶剂浇铸法制备了三种含有不同聚合物量的薄膜配方。对其进行了理化性质、力学性能和粘膜粘附性能以及甲硝唑释放曲线的表征。薄膜表现出的理化性质、力学性能和粘膜粘附特性取决于聚合物的组成和药物的存在。它们能够迅速溶胀并促进药物的快速释放(20 分钟内释放 80%),这是由菲克扩散控制的。薄膜在不到 90 秒内完全崩解,30 分钟内完全释放药物。因此,这些配方为经口腔修饰传递甲硝唑的药物应用提供了一种有前途的替代方案。

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