"Cellular uptake, antioxidant and antiproliferative activity of entrapp" by Saeed Alqahtani, Lacey Simon et al.

Faculty Publications

Title

Cellular uptake, antioxidant and antiproliferative activity of entrapped α-tocopherol and γ-tocotrienol in poly (lactic-co-glycolic) acid (PLGA) and chitosan covered PLGA nanoparticles (PLGA-Chi)

Authors

Saeed Alqahtani, Department of Basic Pharmaceutical Sciences, School of Pharmacy, University of Louisiana at Monroe, 1800 Bienville Dr., Monroe, LA 71201, USA.
Lacey Simon, Department of Biological and Agricultural Engineering, LSU Agricultural Center, Louisiana State University, Baton Rouge, LA 70803, USA.
Carlos E. Astete, Department of Biological and Agricultural Engineering, LSU Agricultural Center, Louisiana State University, Baton Rouge, LA 70803, USA.
Alaadin Alayoubi, Department of Basic Pharmaceutical Sciences, School of Pharmacy, University of Louisiana at Monroe, 1800 Bienville Dr., Monroe, LA 71201, USA.
Paul W. Sylvester, Department of Basic Pharmaceutical Sciences, School of Pharmacy, University of Louisiana at Monroe, 1800 Bienville Dr., Monroe, LA 71201, USA.
Sami Nazzal, Department of Basic Pharmaceutical Sciences, School of Pharmacy, University of Louisiana at Monroe, 1800 Bienville Dr., Monroe, LA 71201, USA.
Yixiao Shen, Department of Biological and Agricultural Engineering, LSU Agricultural Center, Louisiana State University, Baton Rouge, LA 70803, USA.

Document Type

Article

Publication Date

5-1-2015

Abstract

The aim of this study was to formulate and characterize α-tocopherol (α-T) and tocotrienol-rich fraction (TRF) entrapped in poly (lactide-co-glycolide) (PLGA) and chitosan covered PLGA (PLGA-Chi) based nanoparticles. The resultant nanoparticles were characterized and the effect of nanoparticles entrapment on the cellular uptake, antioxidant, and antiproliferative activity of α-T and TRF were tested. In vitro uptake studies in Caco2 cells showed that PLGA and PLGA-Chi nanoparticles displayed a greater enhancement in the cellular uptake of α-T and TRF when compared with the control without causing toxicity to the cells (p < 0.0001). Furthermore, the cellular internalization of both PLGA and PLGA-Chi nanoparticles labeled with FITC was investigated by fluorescence microscopy; both types of nanoparticles were able to get internalized into the cells with reasonable amounts. However, PLGA-Chi nanoparticles showed significantly higher (3.5-fold) cellular uptake compared to PLGA nanoparticles. The antioxidant activity studies demonstrated that entrapment of α-T and TRF in PLGA and PLGA-Chi nanoparticles exhibited greater ability in inhibiting cholesterol oxidation at 48 h compared to the control. In vitro antiproliferative studies confirmed marked cytotoxicity of TRF on MCF-7 and MDA-MB-231 cell lines when delivered by PLGA and PLGA-Chi nanoparticles after 48 h incubation compared to control. In summary, PLGA and PLGA-Chi nanoparticles may be considered as an attractive and promising approach to enhance the bioavailability and activity of poorly water soluble compounds such as α-tocopherol and tocotrienols.

Publication Source (Journal or Book title)

Journal of colloid and interface science

First Page

243

Last Page

251

Recommended Citation

Alqahtani, S., Simon, L., Astete, C. E., Alayoubi, A., Sylvester, P. W., Nazzal, S., & Shen, Y. (2015). Cellular uptake, antioxidant and antiproliferative activity of entrapped α-tocopherol and γ-tocotrienol in poly (lactic-co-glycolic) acid (PLGA) and chitosan covered PLGA nanoparticles (PLGA-Chi). Journal of colloid and interface science, 445, 243-251. https://doi.org/10.1016/j.jcis.2014.12.083

Link to Full Text

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