Imam Syed Sarim, Alshehri Sultan, Altamimi Mohammad A, Hussain Afzal, Alyahya Khaled Hamad, Mahdi Wael A, Qamar Wajhul
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Department of Pharmacology and Toxicology, Central Laboratory, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
ACS Omega. 2021 Dec 23;7(1):1048-1056. doi: 10.1021/acsomega.1c05628. eCollection 2022 Jan 11.
Luteolin (LT) is a natural polyphenol water-insoluble compound. LT-loaded nanovesicles (NVs) were prepared by using the solvent evaporation method. LT-NVs were prepared using cholesterol, phosphatidylcholine, span 60, and labrasol in a different composition. The prepared LT-NVs were evaluated for encapsulation efficiency, in vitro drug release, and permeation study. The optimized LT-NVs were further evaluated for antioxidant activity and cytotoxicity using the lung cancer cell line. LT-NVs showed nanometric size (less than 300 nm), an optimum polydispersibility index (less than 0.5), and a negative zeta potential value. The formulations also showed significant variability in the encapsulation efficiency (69.44 ± 0.52 to 83.75 ± 0.35%) depending upon the formulation composition. The and permeation study results revealed enhanced drug release as well as permeation profile. The formulation LT-NVs (F2) showed the maximum drug release of 88.28 ± 1.13%, while pure LT showed only 20.1 ± 1.21% in 12 h. The release data revealed significant variation ( < 0.001) in the release pattern. The permeation results also depicted significant ( < 0.001) enhancement in the permeation across the membrane. The enhanced permeation from LT-NVs was achieved due to the enhanced solubility of LT in the presence of the surfactant. The antioxidant activity results proved that LT-NVs showed greater activity compared to pure LT. The cytotoxicity study showed lesser IC value from LT-NVs than the pure LT. Thus, it can be concluded that LT-NVs are a natural alternative to the synthetic drug in the treatment of lung cancer.
木犀草素(LT)是一种天然的多酚类水不溶性化合物。采用溶剂蒸发法制备了负载木犀草素的纳米囊泡(NVs)。使用胆固醇、磷脂酰胆碱、司盘60和Labrasol以不同的组成制备了LT-NVs。对制备的LT-NVs进行了包封率、体外药物释放和渗透研究。使用肺癌细胞系对优化后的LT-NVs进一步进行了抗氧化活性和细胞毒性评估。LT-NVs呈现纳米尺寸(小于300nm)、最佳多分散指数(小于0.5)以及负的zeta电位值。根据制剂组成,这些制剂在包封率方面也表现出显著差异(69.44±0.52%至83.75±0.35%)。体外释放和渗透研究结果显示药物释放以及渗透情况均有所增强。制剂LT-NVs(F2)在12小时内的最大药物释放率为88.28±1.13%,而纯LT在12小时内仅释放20.1±1.21%。释放数据显示释放模式存在显著差异(P<0.001)。渗透结果也表明跨膜渗透有显著增强(P<0.001)。由于表面活性剂的存在提高了LT的溶解度,从而实现了LT-NVs的渗透增强。抗氧化活性结果证明,与纯LT相比LT-NVs表现出更强的活性。细胞毒性研究表明,LT-NVs的半数抑制浓度值低于纯LT。因此,可以得出结论,LT-NVs是治疗肺癌的合成药物的天然替代品。