Next Article in Journal
Curcumin, a Natural Antimicrobial Agent with Strain-Specific Activity
Next Article in Special Issue
Profile and Content of Phenolic Compounds in Leaves, Flowers, Roots, and Stalks of Sanguisorba officinalis L. Determined with the LC-DAD-ESI-QTOF-MS/MS Analysis and Their In Vitro Antioxidant, Antidiabetic, Antiproliferative Potency
Previous Article in Journal
Safety of Repeated Administration of Parenteral Ketamine for Depression
Previous Article in Special Issue
A Pilot Study of a Natural Food Supplement as New Possible Therapeutic Approach in Chronic Kidney Disease Patients
Article

Formulation Design, Statistical Optimization, and In Vitro Evaluation of a Naringenin Nanoemulsion to Enhance Apoptotic Activity in A549 Lung Cancer Cells

1
Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia
2
Advanced Drug Delivery Research Group, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia
3
Center of Excellence for Drug Research & Pharmaceutical Industries, King Abdulaziz University, Jeddah 21589, Saudi Arabia
4
Department of Biotechnology, Jamia Millia Islamia (Central University), New Delhi 110025, India
5
Department of Biological Sciences-Cancer Immunology, Faculty of sciences, King Abdulaziz University, Jeddah 21589, Saudi Arabia
6
Department of Natural products and alternative medicine, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia
7
Department of Medical Microbiology and Parasitology, Faculty of Medicine, King Abdulaziz University, Jeddah 21589, Saudi Arabia
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2020, 13(7), 152; https://0-doi-org.brum.beds.ac.uk/10.3390/ph13070152
Received: 30 June 2020 / Revised: 12 July 2020 / Accepted: 13 July 2020 / Published: 15 July 2020
Naringenin (NAR), a flavonoid mainly found in citrus and grapefruits, has proven anti-cancer activities. However, the poor water solubility and low bioavailability of NAR limits its use as a therapeutic agent. The aim of this study was to develop and optimize stable naringenin nanoemulsions (NAR-NE) using a Box–Behnken experimental design to obtain a formulation with a higher efficiency. Anticancer activity of optimized NAR-NE was evaluated in A549 lung cancer cells using cell viability, flow-cytometric assays, and enzyme-linked immunosorbent assay. The stabilized nanoemulsion, which showed a spherical surface morphology, had a globule size of 85.6 ± 2.1 nm, a polydispersity index of 0.263 ± 0.02, a zeta potential of −9.6 ± 1.2 mV, and a drug content of 97.34 ± 1.3%. The NAR release from the nanoemulsion showed an initial burst release followed by a stable and controlled release for a longer period of 24 h. The nanoemulsion exhibited excellent thermodynamic and physical stability against phase separation and storage. The NAR-NE showed concentration-dependent cytotoxicity in A549 lung cancer cells, which was greater than that of free NAR. The percentage of apoptotic cells and cell cycle arrest at the G2/M and pre-G1 phases induced by NAR-NE were significantly higher than those produced by free NAR (p < 0.05). NAR-NEs were more effective than the NAR solution in reducing Bcl2 expression, while increasing pro-apoptotic Bax and caspase-3 activity. Therefore, stabilized NAR-NE could be a suitable drug delivery system to enhance the effects of NAR in the treatment of lung cancer. View Full-Text
Keywords: apoptosis; Box–Behnken design; naringenin; natural product; lung cancer apoptosis; Box–Behnken design; naringenin; natural product; lung cancer
Show Figures

Graphical abstract

MDPI and ACS Style

Md, S.; Alhakamy, N.A.; Aldawsari, H.M.; Husain, M.; Kotta, S.; Abdullah, S.T.; A. Fahmy, U.; Alfaleh, M.A.; Asfour, H.Z. Formulation Design, Statistical Optimization, and In Vitro Evaluation of a Naringenin Nanoemulsion to Enhance Apoptotic Activity in A549 Lung Cancer Cells. Pharmaceuticals 2020, 13, 152. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13070152

AMA Style

Md S, Alhakamy NA, Aldawsari HM, Husain M, Kotta S, Abdullah ST, A. Fahmy U, Alfaleh MA, Asfour HZ. Formulation Design, Statistical Optimization, and In Vitro Evaluation of a Naringenin Nanoemulsion to Enhance Apoptotic Activity in A549 Lung Cancer Cells. Pharmaceuticals. 2020; 13(7):152. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13070152

Chicago/Turabian Style

Md, Shadab, Nabil A. Alhakamy, Hibah M. Aldawsari, Mohammad Husain, Sabna Kotta, Samaa T. Abdullah, Usama A. Fahmy, Mohamed A. Alfaleh, and Hani Z. Asfour 2020. "Formulation Design, Statistical Optimization, and In Vitro Evaluation of a Naringenin Nanoemulsion to Enhance Apoptotic Activity in A549 Lung Cancer Cells" Pharmaceuticals 13, no. 7: 152. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13070152

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop