Department of Chemical Biology and Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Anhui University of Technology, Ma'anshan 243032, People's Republic of China; Biochemical Engineering Research Center, Anhui University of Technology, Ma'anshan 243002, Anhui, People's Republic of China.
Department of Chemical Biology and Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Anhui University of Technology, Ma'anshan 243032, People's Republic of China.
Int J Pharm. 2022 Aug 25;624:121981. doi: 10.1016/j.ijpharm.2022.121981. Epub 2022 Jul 2.
Flavonoids have many positive pharmacological properties, such as antioxidant, antitumor, and anti-inflammatory activities. However, factors such as low water solubility and low dissolution rate limit their use. To overcome their poor solubility, carrier-free apigenin (API) microparticles and nanoparticles were prepared using three types of antisolvent precipitation technologies: supercritical antisolvent (SCF) technology, ultrasonic-assisted liquid antisolvent (UAL) technology, and high-pressure homogenization (HPH) technology. All three technologies can produce uniform tiny particles. However, the API particles obtained using these different techniques show subtle differences in terms of physical and chemical properties and biological activity. The preparation, characterization, and potential use of API microparticles and nanoparticles to improve in vitro release were studied. The resulting API particles were investigated and compared using Fourier-transform infrared spectroscopy, differential scanning calorimetry, X-ray powder diffraction, and scanning electron microscopy. We determined the optimum conditions for SCF, UAL, and HPH technologies to produce API microparticles and nanoparticles. The antioxidant and antitumor properties of the API particles were also investigated. The results demonstrated that the reduced particle size of the APIs prepared via SCF, UAL, and HPH technologies contributed to the enhanced dissolution rate, which in turn enhanced API bioactivity.
类黄酮具有许多积极的药理特性，如抗氧化、抗肿瘤和抗炎活性。然而，低水溶性和低溶解速率等因素限制了它们的应用。为了克服其较差的溶解性，使用三种抗溶剂沉淀技术（超临界抗溶剂（SCF）技术、超声辅助液抗溶剂（UAL）技术和高压匀浆（HPH）技术）制备了无载体芹菜素（API）微球和纳米粒。所有这三种技术都可以产生均匀的微小颗粒。然而，使用这些不同技术获得的 API 颗粒在物理化学性质和生物活性方面表现出细微的差异。研究了 API 微球和纳米粒的制备、表征及其改善体外释放的潜在用途。使用傅里叶变换红外光谱、差示扫描量热法、X 射线粉末衍射和扫描电子显微镜对所得 API 颗粒进行了研究和比较。我们确定了 SCF、UAL 和 HPH 技术生产 API 微球和纳米粒的最佳条件。还研究了 API 颗粒的抗氧化和抗肿瘤特性。结果表明，SCF、UAL 和 HPH 技术制备的 API 颗粒的粒径减小导致溶解速率提高，进而提高了 API 的生物活性。
