pH-Responsive, Hemocompatible, and Non-Toxic Polysaccharide-Based Hydrogel from Seeds of Salvia spinosa L. for Sustained Release of Febuxostat

Herein, a polysaccharide-based hydrogel from seeds of Salvia spinosa (SSH) was evaluated as a pH-responsive, superporous, hemocompatible, non-toxic, and sustained release material. The SSH-based tablets showed pH-dependent swelling (pH 7.4 > 6.8 > 4.5 > 1.2) as well as swelling and de-swelling behavior at pH 7.4 and 1.2, respectively. Sustained release of febuxostat was achieved by mimicking the gastrointestinal tract conditions for 14 h and following the zero-order kinetics and super case-II transport mechanism. Scanning electron microscopy revealed the porous nature of SSH even after compression. SSH was found to be hemocompatible with antioxidant properties. Acute toxicity studies ensured the safety of SSH at a maximum dose level of 2.0 g kg-1 body weight of the animals. SSH was also found as non-irritant to the eye. The histopathology of vital organs did not show any lesions or inflammation. Conclusively, SSH can be considered a safe ingredient for oral, dermal, and ophthalmic formulations.

本研究以刺鼠尾草（Salvia spinosa）种子制备得到多糖基水凝胶（SSH），并对其作为pH响应型、超多孔、血液相容性、无毒且可用于缓释的载体材料进行了评价。以SSH制备的片剂表现出pH依赖性溶胀行为（pH 7.4 > 6.8 > 4.5 > 1.2），且分别在pH 7.4和1.2条件下呈现溶胀与去溶胀特性。通过模拟胃肠道环境实现了非布司他（febuxostat）长达14小时的持续释放，其释放行为符合零级动力学（zero-order kinetics）与超级case-II转运机制。扫描电子显微镜（Scanning Electron Microscopy）结果显示，即使经压片处理后，SSH仍保持多孔结构。研究证实SSH具备血液相容性与抗氧化活性。急性毒性实验表明，当受试动物的最大给药剂量达2.0 g·kg⁻¹体重时，SSH具有良好安全性。此外，SSH对眼部无刺激性。重要脏器的组织病理学检查未观察到任何损伤或炎症反应。综上，SSH可作为安全辅料应用于口服、经皮及眼科制剂中。