Eudragit ® FS 30 D polymeric films containing chondroitin sulfate as candidates for use in coating seeking modified delivery of drugs

ABSTRACT Polymeric films associating different concentrations of Eudragit(r) FS 30 D (EFS) and chondroitin sulfate (CS) were produced by casting for the development of a new target-specific site material. Formed films kept a final polymer mass of 4% (w/v) in the following proportions: EFS 100:00 CS (control), EFS 95:05 CS, EFS 90:10 CS and EFS 80:20 CS. They were analyzed for physical and chemical characteristics using Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and Raman spectroscopy. Furthermore, they were characterized by their water vapor permeability and degree of hydration at different conditions simulating the gastrointestinal tract. No chemical interactions were observed between CS and EFS, suggesting only a physical interaction between them in the different combinations tested. The results suggest that EFS and CS, when combined, may form films that are candidates for coating processes seeking a modified drug delivery, especially due to the synergism between pH dependency and specific biodegradability properties by the colonic microbiota. EFS 90:10 CS proved to be the most suitable for this purpose considering hydration and permeability characteristics of different associations analyzed.

摘要：本研究通过流延法制备了不同配比的Eudragit FS 30 D（以下简称EFS）与硫酸软骨素（chondroitin sulfate，CS）共混聚合物膜，以开发新型靶向特异性载体材料。所制备膜材的总聚合物浓度为4%（质量体积比，w/v），共设置4组配比：EFS 100:0 CS（对照组）、EFS 95:05 CS、EFS 90:10 CS及EFS 80:20 CS。采用傅里叶变换红外光谱（Fourier transform infrared spectroscopy，FTIR）、扫描电子显微镜（scanning electron microscopy，SEM）与拉曼光谱（Raman spectroscopy）对其理化特性进行表征，并通过模拟胃肠道不同环境的水蒸气透过率与水合度分析其性能。结果显示，CS与EFS之间未发生化学相互作用，仅在各测试配比下存在物理共混相互作用。研究表明，EFS与CS共混可形成适用于缓控释给药包衣工艺的候选膜材，其优势主要源于pH响应性与结肠微生物群特异性生物降解性的协同效应。综合分析各测试配比的水合与透过特性，EFS 90:10 CS被证实为最适配该应用场景的膜材。