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.

鼻腔和口腔控释系统的开发 特别强调化学和物理性质的检查 潜在的粘膜粘附聚合物载体。 新型共聚 合成了含有羧基、羟基或离子的制剂 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力。 这些配方 可以以微粒的形式或以 薄微光盘。 它们在水或各种缓冲剂中膨胀 解决方案。 配方中使用的聚合物的特征在于 表面分析、电离度测量和分析 交联特性和溶胀程度。 两个新颖的经历 心理技术用于表征粘膜粘附力 力量。 用于鼻腔和口腔中的粘膜粘附微粒 应用中，使用含有粘蛋白凝胶或鼻腔的流动通道 粘液或带有粘液的舌下组织。 颗粒从 研究粘液表面作为流体流动条件的函数 （气体）穿过该表面。 对于微盘，拉伸测试 使用过程使候选生物粘合剂接触 与粘液混合一段已知的时间，并进一步分离 施力。