Departamento de Ingeniería Química, Biotecnología y Materiales, Facultad de Ciencias Físicas y Matemáticas, Universidad de Chile, Avenida Beaucheff 851, Santiago, Chile; Universidad de Santiago de Chile (USACH), Facultad de Química y Biología, Departamento de Ciencias del Ambiente, Grupo Polímeros, Chile.
Universidad de Santiago de Chile (USACH), Facultad de Química y Biología, Departamento de Ciencias del Ambiente, Grupo Polímeros, Chile.
Int J Biol Macromol. 2022 Feb 28;199:96-107. doi: 10.1016/j.ijbiomac.2021.12.093. Epub 2021 Dec 29.
Several drugs are chemically unstable in the gastric environment and have low bioavailability restricted by intestinal absorption, which motivates the development of alternative routes for drug release, such as transdermal drug carriers for drug delivery to specific areas of the skin. Herein, novel polyelectrolyte complexes (PEC) consisting of carboxymethylagarose (CMA) and chitosan (CS) were prepared. pH-responsive CMA/CS hydrogels were obtained by mixing CMA and CS at various weight ratios. Swelling ratio was modulated by varying the CMA and CS weight ratio, and the highest swelling values were achieved for 2:1 wt% hydrogels at 25 °C and pH 6.0. PEC films were characterized by ATR-FTIR spectroscopy, TGA, DSC, and SEM. Results indicated that CMA and CS were successfully crosslinked by ionic complexation. As a model drug, diclofenac sodium (DS) was loaded in CMA/CS PECs. Association efficiency and loading capacity were ca. 69% and 79%, respectively, exhibiting 67% cumulative release after 72 h at 37 °C and pH 6.0 through Fickian diffusion mechanism. Viability assay of immortalized human keratinocyte (HaCat) cells showed ca. 100% survival in the presence of hydrogels and DS. Therefore, this work suggests that CMA/CS PECs can be applied as pH-responsive carriers for dermal drug delivery.
几种药物在胃环境中化学不稳定，并且肠道吸收受到生物利用度的限制，这促使人们开发了替代的药物释放途径，例如用于将药物递送到皮肤特定区域的透皮药物载体。在此，制备了由羧甲基琼脂糖（CMA）和壳聚糖（CS）组成的新型聚电解质复合物（PEC）。通过以各种重量比混合 CMA 和 CS 来获得 pH 响应性 CMA/CS 水凝胶。通过改变 CMA 和 CS 的重量比来调节溶胀比，在 25°C 和 pH 6.0 下，2:1wt%水凝胶的溶胀值最高。通过 ATR-FTIR 光谱、TGA、DSC 和 SEM 对 PEC 薄膜进行了表征。结果表明，CMA 和 CS 通过离子络合成功交联。将双氯芬酸钠（DS）作为模型药物载入 CMA/CS PEC 中。结合效率和载药量分别约为 69%和 79%，在 37°C 和 pH 6.0 下通过 Fickian 扩散机制 72 小时后累积释放约 67%。永生化人角质形成细胞（HaCat）细胞的活力测定表明，在水凝胶和 DS 的存在下，细胞存活率约为 100%。因此，这项工作表明 CMA/CS PEC 可作为用于皮肤药物递送的 pH 响应性载体。
