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

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.

Automated summary

Luteolin-loaded nanovesicles were successfully prepared using the solvent evaporation method, showing nanometric size, optimum polydispersibility index, and negative zeta potential. These nanovesicles exhibited enhanced drug release and permeation properties, with significant variations in encapsulation efficiency depending on the composition. The antioxidant activity of LT-NVs was superior to pure luteolin, and cytotoxicity studies showed a lower IC50 value, suggesting their potential as a natural alternative for lung cancer treatment.