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

Citation:
Kassem, M. A., M. A. Megahed, S. A. K. Elyazid, and F. I. Abd-Allah, "Enhancing the Therapeutic Efficacy of Tamoxifen Citrate Loaded Span-Based Nano-Vesicles on Human Breast Adenocarcinoma Cells", AAPS PharmSciTech, vol. Vol. 19, issue No. 4, May , pp. 1529-1543, 2018.

Abstract:

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 spanbased
nano-vesicles for delivery to malignant tissues with maximum efficacy. The effect of
three variables on vesicle size (Y1), zeta potential (Y2), entrapment efficiency (Y3) and the
cumulative percent release after 24 h (Y4) 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 Y1, Y2, Y3, and Y4, 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 IC50 values 4.7 ± 1.5
and 44.3 ± 1.3 μg/ml on cancer and normal cells, respectively. While, free Tmx exhibited
lower selectivity (2.5 folds) than optimized nano-vesicles on cancer cells with IC50 values of
9.0 ± 1.1 μg/ml and 22.5 ± 5.3 μg/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.

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