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基于改性果胶和丙烯酸单体的具有潜在药用辅料应用的新型黏附聚合物的设计、表征及初步体外评价。

Design, characterization and preliminary in vitro evaluation of a mucoadhesive polymer based on modified pectin and acrylic monomers with potential use as a pharmaceutical excipient.

机构信息

Departamento de Farmácia e Nutrição, Universidade Federal do Espírito Santo - UFES, Campus Alegre, Avenida Alto Universitário - sem número, CEP: 29.500-000 Guararema, Alegre, ES, Brazil.

Departamento de Materiais, Tecnologias e Processos, Escola de Design, Universidade Estadual de Minas Gerais - UEMG, Belo Horizonte, MG, Brazil.

出版信息

Carbohydr Polym. 2015 May 5;121:372-81. doi: 10.1016/j.carbpol.2014.12.052. Epub 2015 Jan 3.

DOI:10.1016/j.carbpol.2014.12.052
PMID:25659712
Abstract

Bio-based polymers have been reported to have applications in biomedical and pharmaceutical areas. Polysaccharides, especially prepared from plant sources, have served a variety of uses. This work aims to prepare a polymer for use as a pharmaceutical excipient containing a functionalized carbohydrate (pectin) and acrylic monomers (methyl methacrylate, butyl methacrylate and ethyl acrylate) via an emulsion polymerization technique. Carbon double bonds were incorporated into the pectin by reacting this natural polymer with glycidyl methacrylate. The methacrylated pectin was then polymerized with acrylic monomers by emulsion polymerization. The mucoadhesive performance of the materials was investigated by in vitro preliminary assays based on viscometric studies, texture analysis and film wettability. The obtained results showed that the synergistic viscosity increase with greater concentrations of modified pectin. The contact angle decreased, suggesting an increase in the wettability for polymers with large amounts of methacrylated pectin. The addition of mucin in lattices caused an increase in the intermolecular forces and in the work of adhesion. This corroborates the use of pectin as a mucoadhesive excipient for mucoadhesive drug delivery systems.

摘要

生物基聚合物已被报道在生物医学和制药领域有应用。多糖,特别是从植物来源制备的多糖,具有多种用途。本工作旨在通过乳液聚合技术制备一种用作药物赋形剂的聚合物,其含有功能化碳水化合物(果胶)和丙烯酸单体(甲基丙烯酸甲酯、甲基丙烯酸丁酯和丙烯酸乙酯)。通过使这种天然聚合物与甲基丙烯酸缩水甘油酯反应,将碳双键引入果胶中。然后通过乳液聚合将甲基丙烯酰化果胶与丙烯酸单体聚合。通过基于粘度研究、质地分析和薄膜润湿性的体外初步测定来研究材料的粘膜粘附性能。所得结果表明,协同粘度随着改性果胶浓度的增加而增加。接触角减小,表明具有大量甲基丙烯酰化果胶的聚合物的润湿性增加。在格子中添加粘蛋白会增加分子间力和粘附功。这证实了果胶作为用于粘膜粘附药物传递系统的粘膜粘附赋形剂的用途。

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Design, characterization and preliminary in vitro evaluation of a mucoadhesive polymer based on modified pectin and acrylic monomers with potential use as a pharmaceutical excipient.基于改性果胶和丙烯酸单体的具有潜在药用辅料应用的新型黏附聚合物的设计、表征及初步体外评价。
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