Purpose: This study aims to maximize the Pomegranate extract (PE) chemotherapeutic efficacy by loading it in an optimized solid lipid nanoparticles (SLNs) formula. PE is a natural product with potent antioxidant and anticancer activity because of its polyphenols content.
Methods: The influence of independent variables, which were lipid concentra¬tion (X1), surfactant concentration (X2) and cosurfactant concentration (X3), on dependent ones, which were particle size (Y1), polydispersity index (Y2), zeta potential (Y3), entrapment efficiency (Y4) and cumulative % drug release (Y5), were studied and optimized using the Box–Behnken design. Fifteen formulations of PE-SLNs were prepared using hot homogenization followed by ultra-sonication technique. Response surface plots, Pareto charts and mathematical equations were produced to study the impact of independent variables on the dependent quality parameters. The anti-proliferative activity of the optimized formula was then evaluated in three different cancer cell lines, namely, MCF-7, PC-3 and HepG-2, in addition to one normal cell line, HFB-4.
Results: The results demonstrated that the particle sizes ranged from 407.5 to 651.9 nm and the entrapment efficiencies ranged from 56.02 to 65.23%. Interestingly, the 50% inhibitory concentration of the optimized formula had more than a 40-fold improved effect on the cell growth inhibition in comparison with its free counterpart. Furthermore, it was more selective against cancer cells than normal cells particularly in MCF-7 breast cancer cells.
Conclusion: These results proved that nanoencapsulation of PE enhanced its anticancer efficacy. Therefore, our results suggested that a PE-loaded SLNs optimized-formula could be a promis¬ing chemotherapeutic agent.
Mohamed El-Nabarawi– Professor of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo
Noha Badawi– Lecturer of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, The British University in Egypt
Dalia Attia– Professor of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, The British University in Egypt, Cairo
Mohey Elmazar– Professor of Pharmacology and Dean of Faculty of Pharmacy, Faculty of Pharmacy, The British University in Egypt, Cairo
Khalid Elsay– Professor of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia., Cairo