Imam Syed Sarim, Alshehri Sultan, Mahdi Wael A, Alotaibi Ahmed M, Alhwaifi Moath H, Hussain Afzal, Altamimi Mohammad A, Qamar Wajhul
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Pharmaceuticals (Basel). 2022 Dec 8;15(12):1525. doi: 10.3390/ph15121525.
The work aimed to enhance chrysin (CHR) water solubility, dissolution, and in vitro antibacterial as well as cell viability. Chrysin binary, as well as ternary inclusion complex, were prepared using the spray drying method. The influence of an auxiliary component (poloxamer; PLX) was also assessed after being incorporated into the chrysin HP βCD complex (CHR-BC) and formed as a chrysin ternary complex (CHR-TC). The phase solubility investigation was carried out in order to assess the complexation efficiency and stability constant. The samples were assessed for the dissolution test, physicochemical evaluation, antibacterial activity, and cell viability tests were also assessed. The results of the phase solubility investigation showed that the stability constant for the binary system (268 M) was lower than the ternary system (720 M). The complex stability was validated by the greater stability constant value. The dissolution results showed that pure CHR had a limited release of 32.55 ± 1.7% in 60 min, while prepared CHR-TC and CHR-BC both demonstrated maximum CHR releases of 99.03 ± 2.34% and 71.95 ±2.1%, respectively. The dissolution study's findings revealed that the release of CHR was much improved over that of pure CHR. A study using a scanning electron microscope showed that CHR-TC contains more agglomerated and amorphous components. The higher conversion of crystalline CHR into an amorphous form is responsible for the structural alterations that are observed. After complexation, the distinctive peaks of pure CHR changed due to the complexation with HP βCD and PLX. The antimicrobial and cell viability results revealed improved antimicrobial activity as well as a lower IC50 value than pure CHR against the tested anticancer cell line (MCF7).
该研究旨在提高白杨素（CHR）的水溶性、溶出度以及体外抗菌活性和细胞活力。采用喷雾干燥法制备了白杨素二元包合物以及三元包合物。将辅助成分（泊洛沙姆；PLX）加入白杨素HP-β-环糊精复合物（CHR-BC）中形成白杨素三元复合物（CHR-TC）后，还评估了其影响。进行相溶解度研究以评估络合效率和稳定常数。对样品进行了溶出度测试、理化性质评估、抗菌活性评估以及细胞活力测试。相溶解度研究结果表明，二元体系的稳定常数（268 M）低于三元体系（720 M）。较高的稳定常数验证了复合物的稳定性。溶出结果表明，纯CHR在60分钟内的释放率有限，为32.55±1.7%，而制备的CHR-TC和CHR-BC的CHR最大释放率分别为99.03±2.34%和71.95±2.1%。溶出度研究结果表明，CHR的释放较纯CHR有显著改善。扫描电子显微镜研究表明，CHR-TC含有更多的团聚和无定形成分。结晶CHR向无定形形式的较高转化率导致了观察到的结构变化。络合后，由于与HP-β-环糊精和PLX络合，纯CHR的特征峰发生了变化。抗菌和细胞活力结果表明，与纯CHR相比，对测试的抗癌细胞系（MCF7）的抗菌活性有所提高，IC50值更低。
