羟乙基纤维素基水凝胶作为白芍生物活性成分无定形固体分散体的控释载体。
Hydroxyethyl Cellulose-Based Hydrogels as Controlled Release Carriers for Amorphous Solid Dispersion of Bioactive Components of Radix Paeonia Alba.
发表日期:2023 Oct 28
作者:
Abid Naeem, Chengqun Yu, Xiaoli Wang, Mingyan Peng, Yi Liu, Yali Liu
来源:
Stem Cell Research & Therapy
摘要:
白芍 (RPA) 在中药中被广泛用于治疗胃肠道疾病、免疫调节疾病、癌症和许多其他疾病。它的一些活性成分包括芍药苷、白花苷、乳花苷和儿茶素。然而,它们的治疗效果因药代动力学较差、口服生物利用度低、半衰期短和水溶性差而受到影响。本研究成功制备了羟乙基纤维素接枝2-丙烯酰胺-2-甲基丙磺酸(HEC-g-AMPS)水凝胶,用于白芍固体分散体(RPA-SD)的控释。使用 UHPLC-Q-TOF-MS 分析在 RPA-SD 中总共鉴定出 43 种化合物。通过 FTIR、TGA、DSC、XRD 和 SEM 证实了水凝胶网络的形成。 48小时后,水凝胶在pH 1.2时的溶胀和药物释放(溶胀43.31%,药物释放81.70%)略高于pH 7.4时(溶胀27.73%,药物释放72.46%)。水凝胶的凝胶分数、药物释放时间和机械强度随着聚合物和单体浓度的增加而增加。此外,水凝胶是多孔的(孔隙率为 84.15%)且可生物降解(每周减重 8.9%)。此外,合成的水凝胶表现出优异的抗菌和抗氧化性能。
Radix Paeoniae Alba (RPA) has been used extensively in Chinese traditional medicine to treat gastrointestinal disorders, immune-modulating diseases, cancers, and numerous other conditions. A few of its active components include paeoniflorin, albiflorin, lactiflorin, and catechin. However, their therapeutic effectiveness is compromised by poor pharmacokinetic profiles, low oral bioavailability, short half-lives, and poor aqueous solubility. In this study, hydroxyethyl cellulose-grafted-2-acrylamido-2-methylpropane sulfonic acid (HEC-g-AMPS) hydrogels were successfully prepared for the controlled release of Radix Paeonia Alba-solid dispersion (RPA-SD). A total of 43 compounds were identified in RPA-SD using UHPLC-Q-TOF-MS analysis. The hydrogel network formation was confirmed by FTIR, TGA, DSC, XRD, and SEM. Hydrogels' swelling and drug release were slightly higher at pH 1.2 (43.31% swelling, 81.70% drug release) than at pH 7.4 (27.73% swelling, 72.46% drug release) after 48 h. The gel fraction, drug release time and mechanical strength of the hydrogels increased with increased polymer and monomer concentration. Furthermore, the hydrogels were porous (84.15% porosity) and biodegradable (8.9% weight loss per week). Moreover, the synthesized hydrogels exhibited excellent antimicrobial and antioxidative properties.