Nanotheranostics 2021; 5(1):113-124. doi:10.7150/ntno.51955

Research Paper

Resveratrol loaded polymeric micelles for theranostic targeting of breast cancer cells

Yiota Gregoriou1,2,3✉, Gregoria Gregoriou1, Vural Yilmaz1, Konstantinos Kapnisis4, Marianna Prokopi4, Andreas Anayiotos4, Katerina Strati1, Nikolas Dietis5, Andreas I. Constantinou1, Chrysafis Andreou2,3✉

1. Department of Biological Sciences, Faculty of Pure and Applied Sciences, University of Cyprus, Nicosia, Cyprus.
2. Department of Electrical and Computer Engineering University of Cyprus, Nicosia, Cyprus.
3. Emphasis Research Centre, University of Cyprus, Nicosia, Cyprus.
4. Department of Mechanical Engineering and Material Science and Engineering, Cyprus University of Technology, Limassol, Cyprus.
5. Medical School University of Cyprus, Nicosia, Cyprus.

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Citation:
Gregoriou Y, Gregoriou G, Yilmaz V, Kapnisis K, Prokopi M, Anayiotos A, Strati K, Dietis N, Constantinou AI, Andreou C. Resveratrol loaded polymeric micelles for theranostic targeting of breast cancer cells. Nanotheranostics 2021; 5(1):113-124. doi:10.7150/ntno.51955. Available from https://www.ntno.org/v05p0113.htm

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Abstract

Treatment of breast cancer underwent extensive progress in recent years with molecularly targeted therapies. However, non-specific pharmaceutical approaches (chemotherapy) persist, inducing severe side-effects. Phytochemicals provide a promising alternative for breast cancer prevention and treatment. Specifically, resveratrol (res) is a plant-derived polyphenolic phytoalexin with potent biological activity but displays poor water solubility, limiting its clinical use. Here we have developed a strategy for delivering res using a newly synthesized nano-carrier with the potential for both diagnosis and treatment.

Methods: Res-loaded nanoparticles were synthesized by the emulsion method using Pluronic F127 block copolymer and Vitamin E-TPGS. Nanoparticle characterization was performed by SEM and tunable resistive pulse sensing. Encapsulation Efficiency (EE%) and Drug Loading (DL%) content were determined by analysis of the supernatant during synthesis. Nanoparticle uptake kinetics in breast cancer cell lines MCF-7 and MDA-MB-231 as well as in MCF-10A breast epithelial cells were evaluated by flow cytometry and the effects of res on cell viability via MTT assay.

Results: Res-loaded nanoparticles with spherical shape and a dominant size of 179±22 nm were produced. Res was loaded with high EE of 73±0.9% and DL content of 6.2±0.1%. Flow cytometry revealed higher uptake efficiency in breast cancer cells compared to the control. An MTT assay showed that res-loaded nanoparticles reduced the viability of breast cancer cells with no effect on the control cells.

Conclusions: These results demonstrate that the newly synthesized nanoparticle is a good model for the encapsulation of hydrophobic drugs. Additionally, the nanoparticle delivers a natural compound and is highly effective and selective against breast cancer cells rendering this type of nanoparticle an excellent candidate for diagnosis and therapy of difficult to treat mammary malignancies.

Keywords: cancer nanomedicine, nanotheranostics, resveratrol, breast cancer, drug-delivery