MUCOADHESIVE POLYMERS FOR NASAL AND BUCCAL DRUG DELIVERY

用于鼻腔和口腔给药的粘膜粘附聚合物

• 批准号: 3304419
• 负责人: NICHOLAS A PEPPAS
• 金额: $ 10.42万
• 依托单位: PURDUE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1991
• 资助国家: 美国
• 起止时间: 1991-05-01 至 1994-04-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3304419
• 关键词: chemical bond; copolymer; crosslink; drug administration routes; drug delivery systems; drug interactions; hydropathy; mathematical model; mucosa; oral administration; oral mucosa; photoelectron spectrometry; polymers; solutions; water solution

The development of nasal and buccal controlled release systems is examined with special emphasis on the chemical and physical properties of the potentially mucoadhesive polymeric carriers. New copolymeric formulations were synthesized, containing carboxylic, hydroxylic or ionic groups which can interact with mucin solutions, mucin gels or mucosa to provide a relatively permanent mucoadhesive bond. These formulations could be prepared either in the form of microparticles or in the form of thin microdiscs. They were swellable in water or various buffered solutions. The polymers used in the formulations were characterized with surface analysis, measurement of their degree of ionization and analysis of the crosslinked properties and degree of swelling. Two novel experi- mental techniques are used to characterize the mucoadhesive bond strength. For muco-adhesive microparticles both in nasal and buccal applications, a flow channel is used containing a mucin gel or nasal mucus or sublingual tissue with mucus. The particle detachment from the mucus surface is studied as a function of flow conditions of the fluid (gas) passing over this surface. For microdiscs, a tensile testing process is used whereby the candidate bioadhesive is brought in contact with mucus for a known period of time and is further detached by application of force.

鼻腔和口腔控制释放系统的发展是 特别强调了化学和物理性质的研究 潜在的粘膜粘附性聚合物载体。 新型共聚树脂 合成了含有羧基、羟基或离子型的制剂， 可以与粘蛋白溶液、粘蛋白凝胶或粘膜相互作用的基团， 提供相对永久的粘膜粘附结合。 这些制剂 可以以微粒的形式或以 薄的微光盘 它们在水中或各种缓冲溶液中可溶胀 解决方案 制剂中使用的聚合物的特征在于： 表面分析、电离度测量和分析 的交联性能和溶胀度。 两个新的实验- 心理技术用于表征粘膜粘附结合 实力 对于鼻腔和口腔中的粘膜粘附微粒 在一些应用中，使用含有粘蛋白凝胶或鼻粘膜的流动通道。 粘液或含粘液的舌下组织。 颗粒从 粘液表面被研究为流体流动条件的函数 (gas)穿过这个表面。 对于微盘，拉伸测试 使用使候选生物粘附剂接触的方法 与粘液接触一段已知的时间，并通过 使用武力。