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 本研究以流延法制备了不同配比的Eudragit(r) FS 30 D（简称EFS）与硫酸软骨素（chondroitin sulfate，简称CS）共混聚合物膜，用于开发新型靶向部位递送载体材料。所制得的膜体系总聚合物固含量为4%（质量体积比，w/v），各组分配比分别为：EFS 100:00 CS（空白对照组）、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）及拉曼光谱对膜的理化性质进行表征；此外，通过模拟胃肠道环境的不同条件，测定膜的水蒸气透过率与水合度。实验未检测到CS与EFS之间存在化学相互作用，表明在各测试配比下二者仅存在物理共混相互作用。研究结果表明，EFS与CS共混可制备得到适用于缓控释给药包衣工艺的聚合物膜，这一应用潜力主要源于其pH依赖性与结肠微生物群特异性生物降解性之间的协同效应。综合各配比膜的水合特性与透过性能，EFS 90:10 CS配比的膜被证实为该应用场景下的最优选择。