Enhancing the Therapeutic Efficacy of Tamoxifen Citrate Loaded Span-Based Nano-Vesicles on Human Breast Adenocarcinoma Cells

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From: AAPS PharmSciTech(Vol. 19, Issue 4)
Publisher: Springer
Document Type: Report
Length: 403 words

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To access, purchase, authenticate, or subscribe to the full-text of this article, please visit this link: http://dx.doi.org/10.1208/s12249-018-0962-y Byline: Mohammed A. Kassem (1), Mohamed A. Megahed (2), Sherif K. Abu Elyazid (2,3), Fathy I. Abd-Allah (2,3), Tamer M. Abdelghany (4), Ahmed M. Al-Abd (5,6,7), Khalid M. El-Say (3,8) Keywords: Box-Behnken design; Breast cancer cells; In vitro cytotoxicity; Optimization; Tamoxifen citrate Abstract: Serious adverse effects and low selectivity to cancer cells are the main obstacles of long term therapy with Tamoxifen (Tmx). This study aimed to develop Tmx-loaded span-based nano-vesicles for delivery to malignant tissues with maximum efficacy. The effect of three variables on vesicle size (Y.sub.1), zeta potential (Y.sub.2), entrapment efficiency (Y.sub.3) and the cumulative percent release after 24 h (Y.sub.4) were optimized using Box-Behnken design. The optimized formula was prepared and tested for its stability in different storage conditions. The observed values for the optimized formula were 310.2 nm, -42.09 mV, 75.45 and 71.70% for Y.sub.1, Y.sub.2, Y.sub.3, and Y.sub.4, respectively. The examination using electron microscopy confirmed the formation of rounded vesicles with distinctive bilayer structure. Moreover, the cytotoxic activity of the optimized formula on both breast cancer cells (MCF-7) and normal cells (BHK) showed enhanced selectivity (9.4 folds) on cancerous cells with IC.sub.50 values 4.7[+ or -]1.5 and 44.3[+ or -]1.3 [micro]g/ml on cancer and normal cells, respectively. While, free Tmx exhibited lower selectivity (2.5 folds) than optimized nano-vesicles on cancer cells with IC.sub.50 values of 9.0[+ or -]1.1 [micro]g/ml and 22.5[+ or -]5.3 [micro]g/ml on MCF-7 and BHK cells, respectively. The promising prepared vesicular system, with greater efficacy and selectivity, provides a marvelous tool to overcome breast cancer treatment challenges. Author Affiliation: (1) 0000 0004 0639 9286, grid.7776.1, Department of Pharmaceutics and Industrial Pharmacy, Cairo University, Cairo, Egypt (2) grid.442695.8, Department of Pharmaceutics and Pharmaceutical Technology, Egyptian Russian University, Cairo, Egypt (3) 0000 0001 2155 6022, grid.411303.4, Department of Pharmaceutics and Industrial Pharmacy, Al-Azhar University, Cairo, Egypt (4) 0000 0001 2155 6022, grid.411303.4, Department of Pharmacology and Toxicology, Al-Azhar University, Cairo, Egypt (5) 0000 0001 0619 1117, grid.412125.1, Department of Pharmacology and Toxicology, King Abdulaziz University, Jeddah, Saudi Arabia (6) 0000 0001 2151 8157, grid.419725.c, Pharmacology Department, Medical Division, National Research Center, Giza, Egypt (7) Biomedical Research Section, Nawah Scientific, Cairo, Egypt (8) 0000 0001 0619 1117, grid.412125.1, Department of Pharmaceutics, King Abdulaziz University, Jeddah, Saudi Arabia Article History: Registration Date: 24/01/2018 Received Date: 07/11/2017 Accepted Date: 23/01/2018 Online Date: 22/02/2018

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Gale Document Number: GALE|A537723947