Formulation and Evaluation of Luteolin-Loaded Nanovesicles: In Vitro Physicochemical Characterization and Viability Assessment

被引:20
|
作者
Imam, Syed Sarim [1 ]
Alshehri, Sultan [1 ]
Altamimi, Mohammad A. [1 ]
Hussain, Afzal [1 ]
Alyahya, Khaled Hamad [1 ]
Mahdi, Wael A. [1 ]
Qamar, Wajhul [2 ]
机构
[1] King Saud Univ, Coll Pharm, Dept Pharmaceut, Riyadh 11451, Saudi Arabia
[2] King Saud Univ, Coll Pharm, Dept Pharmacol & Toxicol, Cent Lab, Riyadh 11451, Saudi Arabia
来源
ACS OMEGA | 2022年 / 7卷 / 01期
关键词
ORAL BIOAVAILABILITY; NIOSOMES; DELIVERY; DESIGN;
D O I
10.1021/acsomega.1c05628
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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 in vitro 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 (p < 0.001) in the release pattern. The permeation results also depicted significant (p < 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 IC50 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.
引用
收藏
页码:1048 / 1056
页数:9
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