School of Ocean and Tropical Medicine, Research Center of Nano Technology and Application Engineering, Guangdong Medical University, Zhanjiang 524023, China.
Zhanjiang Institute for Drug Control, Zhanjiang 524023, China.
Molecules. 2024 Jun 6;29(11):2693. doi: 10.3390/molecules29112693.
Curcumin (Cur) is a phytochemical with various beneficial properties, including antioxidant, anti-inflammatory, and anticancer activities. However, its hydrophobicity, poor bioavailability, and stability limit its application in many biological approaches. In this study, a novel amphiphilic chitosan wall material was synthesized. The process was carried out via grafting chitosan with succinic anhydride (SA) as a hydrophilic group and deoxycholic acid (DA) as a hydrophobic group; H-NMR, FTIR, and XRD were employed to characterize the amphiphilic chitosan (CS-SA-DA). Using a low-cost, inorganic solvent-based procedure, CS-SA-DA was self-assembled to load Cur nanomicelles. This amphiphilic polymer formed self-assembled micelles with a core-shell structure and a critical micelle concentration (CMC) of 0.093 mg·mL. Cur-loaded nanomicelles were prepared by self-assembly and characterized by the Nano Particle Size Potential Analyzer and transmission electron microscopy (TEM). The mean particle size of the spherical Cur-loaded micelles was 770 nm. The drug entrapment efficiency and loading capacities were up to 80.80 ± 0.99% and 19.02 ± 0.46%, respectively. The in vitro release profiles of curcumin from micelles showed a constant release of the active drug molecule. Cytotoxicity studies and toxicity tests for zebrafish exhibited the comparable efficacy and safety of this delivery system. Moreover, the results showed that the entrapment of curcumin in micelles improves its stability, antioxidant, and anti-inflammatory activity.
姜黄素（Cur）是一种具有多种有益特性的植物化学物质，包括抗氧化、抗炎和抗癌活性。然而，其疏水性、生物利用度差和稳定性限制了它在许多生物学方法中的应用。在这项研究中，合成了一种新型的两亲性壳聚糖壁材料。该过程通过将壳聚糖与琥珀酸酐（SA）作为亲水性基团和脱氧胆酸（DA）作为疏水性基团接枝来进行；采用 H-NMR、FTIR 和 XRD 对两亲性壳聚糖（CS-SA-DA）进行了表征。使用低成本、基于无机溶剂的程序，CS-SA-DA 自组装负载姜黄素纳米胶束。这种两亲性聚合物形成了具有核壳结构和临界胶束浓度（CMC）为 0.093 mg·mL 的自组装胶束。通过自组装制备载姜黄素的纳米胶束，并通过纳米颗粒大小电位分析仪和透射电子显微镜（TEM）进行表征。载姜黄素的球形胶束的平均粒径为 770nm。药物包封效率和载药量分别高达 80.80±0.99%和 19.02±0.46%。从胶束中释放姜黄素的体外释放曲线显示出活性药物分子的持续释放。细胞毒性研究和斑马鱼毒性试验表明，该递药系统具有相当的疗效和安全性。此外，结果表明，姜黄素包封在胶束中提高了其稳定性、抗氧化和抗炎活性。
