Adami Renata, Russo Paola, Amante Chiara, De Soricellis Chiara, Della Porta Giovanna, Reverchon Ernesto, Del Gaudio Pasquale
Department of Physics E. Caianiello, University of Salerno, Via Giovanni Paolo II, 132, 84084 Fisciano, SA, Italy.
Department of Pharmacy, University of Salerno, Via Giovanni Paolo II, 132, 84084 Fisciano, SA, Italy.
Pharmaceutics. 2022 Aug 3;14(8):1623. doi: 10.3390/pharmaceutics14081623.
Flavonoids are polyphenolic compounds largely present in fruits and vegetables possessing antioxidant properties, anti-inflammatory and antibacterial activities. Their use in clinical practice is very poor due to their low bioavailability, susceptibility to oxidation and degradation. Moreover, their slight solubility in biological fluids and a consequent low dissolution rate leads to an irregular absorption from solid dosage forms, even though, anti-inflammatory formulations could be used as support for several disease treatment, i.e. the COVID-19 syndrome. To improve flavonoid bioavailability particle size of the powder can be reduced to make it breathable and to promote the absorption in the lung tissues. Supercritical fluid based antisolvent technique has been used to produce naringin particles, with size, shape and density as well as free flowing properties able to fit inhalation needs. The dried particles are produced with the removal of the solvent at lower temperatures compared to the most used traditional micronization processes, such as spray drying. The best breathable fraction for naringin particles is obtained for particles with a d~7 µm manufactured at 35 °C-150 bar and at 60 °C-130 bar, corresponding to 32.6% and 36.7% respectively. The powder is produced using a high CO molar fraction (0.99) that assure a better removal of the solvent. NuLi-1 cell line of immortalised bronchial epithelial cells adopted to evaluate powder cytotoxicity indicated after 24 h absence of toxicity at concentration of 25 µM.
黄酮类化合物是一类多酚化合物，大量存在于具有抗氧化、抗炎和抗菌活性的水果和蔬菜中。由于其生物利用度低、易氧化和降解，它们在临床实践中的应用非常有限。此外，它们在生物流体中的溶解度低，导致溶解速率低，从而使固体剂型的吸收不规则，尽管抗炎制剂可用于支持多种疾病的治疗，如新冠综合征。为了提高黄酮类化合物的生物利用度，可以减小粉末的粒径，使其具有透气性，并促进在肺组织中的吸收。基于超临界流体的抗溶剂技术已被用于制备柚皮苷颗粒，其尺寸、形状、密度以及自由流动特性能够满足吸入需求。与最常用的传统微粉化工艺（如喷雾干燥）相比，干燥颗粒是在较低温度下去除溶剂而产生的。对于在35°C - 150 bar和60°C - 130 bar条件下制造的粒径约为7 µm的颗粒，分别获得了32.6%和36.7%的最佳柚皮苷颗粒透气率。该粉末是使用高CO摩尔分数（0.99）生产的，这确保了更好地去除溶剂。用于评估粉末细胞毒性的永生化支气管上皮细胞NuLi - 1细胞系表明，在25 µM浓度下24小时后无毒性。
