Guangdong Provincial Key Laboratory of Aquatic Product Processing and Safety, Guangdong Province Engineering Laboratory for Marine Biological Products, Guangdong Provincial Engineering Technology Research Center of Seafood, Guangdong Provincial Science and Technology Innovation Center for Subtropical Fruit and Vegetable Processing, College of Food Science and Technology, Guangdong Ocean University, Zhanjiang 524088, China.
Guangdong Province Key Laboratory of Aquatic Products Processing and Safety, Guangdong Province Engineering Laboratory for Marine Biological Products, School of Food Science and Technology, Guangdong Ocean University, Zhanjiang 524088, China.
Mar Drugs. 2022 Feb 12;20(2):136. doi: 10.3390/md20020136.
Chitosan/alginate nanoparticles (DG1-NPs and DG1/Cur-NPs) aiming to enhance the oral antithrombotic activity of clam heparinoid DG1 were prepared by ionotropic pre-gelation. The influence of parameters, such as the concentration of sodium alginate (SA), chitosan (CTS), CaCl, clam heparinoid DG1, and curcumin (Cur), on the characteristics of the nanoparticles, were investigated. Results indicate that chitosan and alginate can be used as polymer matrices to encapsulate DG1, and nanoparticle characteristics depend on the preparation parameters. Nano-particles should be prepared using 0.6 mg/mL SA, 0.33 mg/mL CaCl, 0.6 mg/mL CTS, 7.2 mg/mL DG1, and 0.24 mg/mL Cur under vigorous stirring to produce DG1-NPS and DG1/Cur-NPS with small size, high encapsulation efficiency, high loading capacity, and negative zeta potential from approximately -20 to 30 mV. Data from scanning electron microscopy, Fourier-transform infrared spectrometry, and differential scanning calorimetry analyses showed no chemical reaction between DG1, Cur, and the polymers; only physical mixing. Moreover, the drug was loaded in the amorphous phase within the nanoparticle matrix. In the acute pulmonary embolism murine model, DG1-NPs enhanced the oral antithrombotic activity of DG1, but DG1/Cur-NPs did not exhibit higher antithrombotic activity than DG1-NPs. Therefore, the chitosan/alginate nanoparticles enhanced the oral antithrombotic activity of DG1, but curcumin did not further enhance this effect.
壳聚糖/海藻酸钠纳米粒子（DG1-NPs 和 DG1/Cur-NPs）旨在通过离子预凝胶化来提高贻贝硫酸皮肤素 DG1 的口服抗血栓活性。研究了参数，如海藻酸钠（SA）、壳聚糖（CTS）、CaCl、贻贝硫酸皮肤素 DG1 和姜黄素（Cur）的浓度对纳米粒子特性的影响。结果表明，壳聚糖和海藻酸钠可用作包封 DG1 的聚合物基质，纳米粒子特性取决于制备参数。纳米粒子应在剧烈搅拌下使用 0.6mg/mL 的 SA、0.33mg/mL 的 CaCl、0.6mg/mL 的 CTS、7.2mg/mL 的 DG1 和 0.24mg/mL 的 Cur 制备，以产生粒径小、包封效率高、载药量高、zeta 电位为负约-20 至 30mV 的 DG1-NPS 和 DG1/Cur-NPS。扫描电子显微镜、傅里叶变换红外光谱和差示扫描量热法分析数据表明，DG1、Cur 和聚合物之间没有化学反应；只有物理混合。此外，药物以无定形相负载在纳米粒子基质内。在急性肺栓塞小鼠模型中，DG1-NPs 增强了 DG1 的口服抗血栓活性，但 DG1/Cur-NPs 并未表现出比 DG1-NPs 更高的抗血栓活性。因此，壳聚糖/海藻酸钠纳米粒子增强了 DG1 的口服抗血栓活性，但姜黄素没有进一步增强这种效果。
