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Andima, Moses; Costabile, Gabriella; Isert, Lorenz; Ndakala, Albert J.; Derese, Solomon and Merkel, Olivia M. (2018): Evaluation of beta-Sitosterol Loaded PLGA and PEG-PLA Nanoparticles for Effective Treatment of Breast Cancer: Preparation, Physicochemical Characterization, and Antitumor Activity. In: Pharmaceutics, Vol. 10, No. 4, 232 [PDF, 3MB]

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beta-Sitosterol (beta-Sit) is a dietary phytosterol with demonstrated anticancer activity against a panel of cancers, but its poor solubility in water limits its bioavailability and therapeutic efficacy. In this study, poly(lactide-co-glycolic acid) (PLGA) and block copolymers of poly(ethylene glycol)-block-poly(lactic acid) (PEG-PLA) were used to encapsulate (beta-Sit into nanoparticles with the aim of enhancing its in vitro anticancer activity. beta-Sitosterol-loaded PLGA and PEG-PLA nanoparticles (beta-Sit-PLGA and (beta-Sit-PEG-PLA) were prepared by using a simple emulsion-solvent evaporation technique. The nanoparticles were characterized for size, particle size distribution, surface charge, and encapsulation efficiency. Their cellular uptake and antiproliferative activity was evaluated against MCF-7 and MDA-MB-231 human breast cancer cells using flow cytometry and MTT assays, respectively. (beta-Sit-PLGA and (beta-Sit-PEG-PLA nanoparticles were spherical in shape with average particle sizes of 215.0 +/- 29.7 and 240.6 +/- 23.3 nm, a zeta potential of -13.8 +/- 1.61 and -23.5 +/- 0.27 mV, respectively, and with narrow size distribution. The encapsulation efficiency of (beta-Sit was 62.89 +/- 4.66 and 51.83 +/- 19.72 % in PLGA and PEG-PLA nanoparticles, respectively. In vitro release in phosphate-buffered saline (PBS) and PBS/with 0.2% Tween 20 showed an initial burst release, followed by a sustained release for 408 h. (beta-Sit-PLGA nanoparticles were generally stable in a protein-rich medium, whereas (beta-Sit-PEG-PLA nanoparticles showed a tendency to aggregate. Flow cytometry analysis (FAGS) indicated that (beta-Sit-PLGA nanoparticles were efficiently taken up by the cells in contrast to (beta-Sit-PEG-PLA nanoparticles. (beta-Sit-PLGA nanoparticles were therefore selected to evaluate antiproliferative activity. Cell viability was inhibited by up to 80% in a concentration range of 6.64-53.08 mu g/mL compared to the untreated cells. Taken together, encapsulation of beta-Sitosterol in PLGA nanoparticles is a promising strategy to enhance its anticancer activity against breast cancer cells.

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