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Article

Evaluation of β-Sitosterol Loaded PLGA and PEG-PLA Nanoparticles for Effective Treatment of Breast Cancer: Preparation, Physicochemical Characterization, and Antitumor Activity

1
Department of Pharmacy, Pharmaceutical Technology & Biopharmaceutics, Ludwig-Maximilian University of Munich, Butenandtstr. 5-13, 81377 Munich, Germany
2
Department of Chemistry, University of Nairobi, P.O. Box 30197-00100, Nairobi, Kenya
3
Department of Chemistry, Busitema University, P.O. Box 236, Tororo, Uganda
*
Author to whom correspondence should be addressed.
Pharmaceutics 2018, 10(4), 232; https://doi.org/10.3390/pharmaceutics10040232
Received: 28 September 2018 / Revised: 31 October 2018 / Accepted: 8 November 2018 / Published: 15 November 2018
(This article belongs to the Special Issue Micro and Nano Encapsulation Techniques)
β-Sitosterol (β-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 β-Sit into nanoparticles with the aim of enhancing its in vitro anticancer activity. β-Sitosterol-loaded PLGA and PEG-PLA nanoparticles (β-Sit-PLGA and β-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. β-Sit-PLGA and β-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 β-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. β-Sit-PLGA nanoparticles were generally stable in a protein-rich medium, whereas β-Sit-PEG-PLA nanoparticles showed a tendency to aggregate. Flow cytometry analysis (FACS) indicated that β-Sit-PLGA nanoparticles were efficiently taken up by the cells in contrast to β-Sit-PEG-PLA nanoparticles. β-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 μg/mL compared to the untreated cells. Taken together, encapsulation of β-Sitosterol in PLGA nanoparticles is a promising strategy to enhance its anticancer activity against breast cancer cells. View Full-Text
Keywords: β-Sitosterol; PLGA nanoparticles; PEG-PLA nanoparticles; breast cancer β-Sitosterol; PLGA nanoparticles; PEG-PLA nanoparticles; breast cancer
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MDPI and ACS Style

Andima, M.; Costabile, G.; Isert, L.; Ndakala, A.J.; Derese, S.; Merkel, O.M. Evaluation of β-Sitosterol Loaded PLGA and PEG-PLA Nanoparticles for Effective Treatment of Breast Cancer: Preparation, Physicochemical Characterization, and Antitumor Activity. Pharmaceutics 2018, 10, 232. https://doi.org/10.3390/pharmaceutics10040232

AMA Style

Andima M, Costabile G, Isert L, Ndakala AJ, Derese S, Merkel OM. Evaluation of β-Sitosterol Loaded PLGA and PEG-PLA Nanoparticles for Effective Treatment of Breast Cancer: Preparation, Physicochemical Characterization, and Antitumor Activity. Pharmaceutics. 2018; 10(4):232. https://doi.org/10.3390/pharmaceutics10040232

Chicago/Turabian Style

Andima, Moses, Gabriella Costabile, Lorenz Isert, Albert J. Ndakala, Solomon Derese, and Olivia M. Merkel. 2018. "Evaluation of β-Sitosterol Loaded PLGA and PEG-PLA Nanoparticles for Effective Treatment of Breast Cancer: Preparation, Physicochemical Characterization, and Antitumor Activity" Pharmaceutics 10, no. 4: 232. https://doi.org/10.3390/pharmaceutics10040232

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