Matchimabura Nattawipa, Poolsiri Jiramate, Phadungvitvatthana Nataporn, Praparatana Rachanida, Issarachot Ousanee, Wiwattanapatapee Ruedeekorn
Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Songkhla 90112, Thailand.
Faculty of Medical Technology, Prince of Songkla University, Songkhla 90112, Thailand.
Polymers (Basel). 2025 Aug 25;17(17):2301. doi: 10.3390/polym17172301.
Ferulic acid (FA) is a bioactive compound known for its potent antioxidant and anti-inflammatory properties; however, its poor water solubility significantly limits its bioavailability and therapeutic potential. In this study, a solid dispersion of FA (FA-SD) was developed using Eudragit EPO via the solvent evaporation method, achieving a 24-fold increase in solubility (42.7 mg/mL) at a 1:3 drug-to-polymer ratio. Expandable gastroretentive films were subsequently formulated using starches from Hom-Nil rice, glutinous rice, and white rice, combined with chitosan as the primary film-forming agents, via the solvent casting technique. Hydroxypropyl methylcellulose (HPMC) K100 LV was incorporated as an adjuvant to achieve controlled release. At optimal concentrations (3% / starch, 2% / chitosan, and 2% / HPMC), the films exhibited favorable mechanical properties, swelling capacity, and unfolding behavior. Sustained release of FA over 8 h was achieved in formulations containing HPMC with either Hom-Nil or glutinous rice starch. Among the tested formulations (R6, G6, and H6), those incorporating Hom-Nil rice starch demonstrated the most significant antioxidant (10.38 ± 0.23 μg/mL) and anti-inflammatory (9.26 ± 0.14 μg/mL) effects in murine macrophage cell line (RAW 264.7), surpassing the activities of both free FA and FA-SD. These results highlight the potential of anthocyanin-rich pigmented rice starch-based expandable films as effective gastroretentive systems for enhanced FA delivery.
阿魏酸（FA）是一种具有生物活性的化合物，以其强大的抗氧化和抗炎特性而闻名；然而，其较差的水溶性显著限制了其生物利用度和治疗潜力。在本研究中，通过溶剂蒸发法使用Eudragit EPO制备了阿魏酸固体分散体（FA-SD），在药物与聚合物比例为1:3时，溶解度提高了24倍（42.7 mg/mL）。随后，通过溶剂浇铸技术，使用霍姆-尼尔大米、糯米和白米的淀粉与壳聚糖作为主要成膜剂，制备了可膨胀胃滞留膜。加入羟丙基甲基纤维素（HPMC）K100 LV作为辅料以实现控释。在最佳浓度（3%/淀粉、2%/壳聚糖和2%/HPMC）下，这些膜表现出良好的机械性能、溶胀能力和展开行为。在含有HPMC以及霍姆-尼尔或糯米淀粉的制剂中，FA实现了8小时的持续释放。在测试的制剂（R6、G6和H6）中，含有霍姆-尼尔大米淀粉的制剂在小鼠巨噬细胞系（RAW 264.7）中表现出最显著的抗氧化（10.38±0.23μg/mL）和抗炎（9.26±0.14μg/mL）作用，超过了游离FA和FA-SD的活性。这些结果突出了富含花青素的有色大米淀粉基可膨胀膜作为增强FA递送的有效胃滞留系统的潜力。
