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Article

Optimized Icariin Phytosomes Exhibit Enhanced Cytotoxicity and Apoptosis-Inducing Activities in Ovarian Cancer Cells

1
Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia
2
Center of Excellence for Drug Research and Pharmaceutical Industries, King Abdulaziz University, Jeddah 21589, Saudi Arabia
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King Fahd Medical Research Center, King Abdulaziz University, Jeddah 21589, Saudi Arabia
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Advanced drug delivery research group, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia
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Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt
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Department of Medical Microbiology and Parasitology, Faculty of Medicine, King Abdulaziz University, Jeddah 21589, Saudi Arabia
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Department of Biological Sciences, Faculty of Science, King Abdulaziz University, Jeddah 21579, Saudi Arabia
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Department of Pharmacology and Toxicology, Faculty of Pharmacy, King Abdulaziz University, Jeddah, 21589, Saudi Arabia
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Department of Clinical Biochemistry, Faculty of Medicine, King Abdulaziz University, Jeddah 21589, Saudi Arabia
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Department of Pharmaceutics, Faculty of Pharmacy, Jouf University, Skaka 2014, Saudi Arabia
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Department of Pharmaceutics and Industrial Pharmacy, Military Medical Academy, Cairo 11757, Egypt
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(4), 346; https://doi.org/10.3390/pharmaceutics12040346
Received: 25 March 2020 / Revised: 6 April 2020 / Accepted: 9 April 2020 / Published: 11 April 2020
Icariin (ICA) is a flavonol glycoside that has pleiotropic pharmacological actions. It has cytotoxic effects against ovarian cancer cells and increases their chemosensitivity to chemotherapeutic drugs. Phytosomes are identified for their potential in drug delivery of cytotoxic agents. Thus, the purpose of this study was to determine the potential enhancement of ICA cytotoxicity activity in OVCAR-3 ovarian cancer cells via its formulation in phytosomes. ICA-phytosomal formulation was optimized using a Box–Behnken design. Particle size, shape, and in vitro drug release were used to characterize the optimized formula. The optimized formulation exhibited enhanced in vitro drug release. ICA-phytosomes exhibited enhanced cytotoxicity against ovarian cancer cells. Cell cycle analysis indicated accumulation of cells challenged with ICA-phytosomes in G2/M and pre-G1 phases. Staining of cells with annexin V indicated significant elevation of percentage cells with early and late apoptosis as well as total cell death. In addition, the formulation significantly disturbed mitochondrial membrane potential and cellular content of caspase 3. In addition, intracellular release of reactive oxygen species (ROS) was enhanced by ICA-phytosomes. In conclusion, phytosome formulation of ICA significantly potentiates its cytotoxic activities against OVCAR-3 cells. This is mediated, at least partly, by enhanced ICA cellular permeation, apoptosis, and ROS. View Full-Text
Keywords: apoptosis; caspase; icariin; phytosomes; reactive oxygen species apoptosis; caspase; icariin; phytosomes; reactive oxygen species
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MDPI and ACS Style

Alhakamy, N.A.; A. Fahmy, U.; Badr-Eldin, S.M.; Ahmed, O.A.A.; Asfour, H.Z.; Aldawsari, H.M.; Algandaby, M.M.; Eid, B.G.; Abdel-Naim, A.B.; Awan, Z.A.; K. Alruwaili, N.; Mohamed, A.I. Optimized Icariin Phytosomes Exhibit Enhanced Cytotoxicity and Apoptosis-Inducing Activities in Ovarian Cancer Cells. Pharmaceutics 2020, 12, 346. https://doi.org/10.3390/pharmaceutics12040346

AMA Style

Alhakamy NA, A. Fahmy U, Badr-Eldin SM, Ahmed OAA, Asfour HZ, Aldawsari HM, Algandaby MM, Eid BG, Abdel-Naim AB, Awan ZA, K. Alruwaili N, Mohamed AI. Optimized Icariin Phytosomes Exhibit Enhanced Cytotoxicity and Apoptosis-Inducing Activities in Ovarian Cancer Cells. Pharmaceutics. 2020; 12(4):346. https://doi.org/10.3390/pharmaceutics12040346

Chicago/Turabian Style

Alhakamy, Nabil A., Usama A. Fahmy, Shaimaa M. Badr-Eldin, Osama A.A. Ahmed, Hani Z. Asfour, Hibah M. Aldawsari, Mardi M. Algandaby, Basma G. Eid, Ashraf B. Abdel-Naim, Zuhier A. Awan, Nabil K. Alruwaili, and Amir I. Mohamed 2020. "Optimized Icariin Phytosomes Exhibit Enhanced Cytotoxicity and Apoptosis-Inducing Activities in Ovarian Cancer Cells" Pharmaceutics 12, no. 4: 346. https://doi.org/10.3390/pharmaceutics12040346

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