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复配不同比例的Eudragit® FS 30 D（EFS）与硫酸软骨素（Chondroitin Sulfate，CS）的聚合物薄膜，以开发新型靶向特异性给药材料。所制得的薄膜最终聚合物质量体积浓度均为4%（w/v），且按以下质量比复配：EFS 100:00 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）与拉曼光谱对其理化特性进行表征；同时，通过模拟胃肠道的不同环境条件，测定其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，表明在所有测试的复配组合中，二者仅存在物理相互作用。研究结果显示，EFS与CS复配后可形成适用于改良型药物递送包衣工艺的薄膜，这一优势尤其得益于其pH依赖性与结肠菌群特异性生物降解性之间的协同效应。综合分析各复配体系的水合与透过特性，EFS 90:10 CS被证实为最适配该应用目的的最优配方。