Green Nanoemulsion Stabilized by In Situ Self-Assembled Natural Oil/Native Cyclodextrin Complexes: An Eco-Friendly Approach for Enhancing Anticancer Activity of Costunolide against Lung Cancer Cells.

Nabil A Alhakamy,Usama A Fahmy,Wesam H Abdulaal,Mohamed A Alfaleh,Shaimaa M Badr-Eldin,Solomon Z Okbazghi,Osama A A Ahmed,Thikryat Neamatallah,Hibah M Aldawsari,Omar D Al-Hejaili

doi:10.3390/pharmaceutics14020227

Abstract

Lung cancer is the second-most deadly malignancy worldwide, of which smoking is considered a major risk factor and causes 75–80% of lung cancer-related deaths. Costunolide (CTD) extracted from plant species Saussurea, Aucklandia, and Inula exhibits potent anticancer properties, specifically in lung cancer and leukemia. Several nanoemulsions were prepared and optimized using a three-factor Box–Behnken experimental design. The optimized green nanoemulsion (GNE) showed a vesicle size of 199.56 nm. The IC50 values revealed that A549 cells were significantly more sensitive to the optimized CTD formula than the plain formula and raw CTD. A cell cycle analysis revealed that the optimized CTD formula treatment resulted in significant cell cycle arrest at the S phase. The results also indicated that treatment with the CTD formula significantly increased caspase-3, Bax, Bcl-2, and p53 mRNA expression compared to the plain formula and CTD raw. In terms of the inflammatory markers, the optimized formula significantly reduced the activity of TNF-α and NF-κB in comparison with the plain formula and raw drug only. Overall, the findings from the study proved that a CTD GNE formulation could be a promising therapeutic approach for the treatment of lung cancer.

Highlights

According to the World Health Organization’s (WHO) estimated top 20 causes of death in 2016, cancer was listed as the first [1]
According to the WHO, lung cancer is classified as non-small cell lung cancer (NSCLC), which represents 85%, and small cell lung cancer (SCLC), which represents
To determine whether the casp volved in CTD-green nanoemulsion (GNE)-induced apoptosis, we examined the expression of casp

Summary

Introduction

According to the World Health Organization’s (WHO) estimated top 20 causes of death in 2016, cancer was listed as the first [1]. Lung cancer is the main cause of cancer-related death among men, especially in developed countries, and it is becoming more common among women [2]. 2008, 1.6 million new cases of lung cancer were reported in 91 countries around world, and. 1.4 million deaths were documented as a result of lung cancer in 17 countries [4]. Many environmental and lifestyle factors lead to developing lung cancer, cigarette smoking habits are strongly attached to the incidence of lung cancer and its mortality rate [5,6]. According to the WHO, lung cancer is classified as non-small cell lung cancer (NSCLC), which represents 85%, and small cell lung cancer (SCLC), which represents

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Conclusion