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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Resveratrol loaded polymeric micelles for theranostic targeting of breast cancer cells
Yiota Gregoriou1,2,3, Gregoria Gregoriou1, Vural Yilmaz1
1Department of Biological Sciences, Faculty of Pure and Applied Sciences, University of Cyprus, Nicosia, Cyprus.
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.
Insights
This study developed novel nanoparticles to deliver resveratrol (res), a natural compound, effectively targeting breast cancer cells. The res-loaded nanoparticles show high efficacy and selectivity, offering a promising alternative to chemotherapy.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Pharmacology
Background:
- Breast cancer treatment faces challenges with chemotherapy's severe side-effects.
- Phytochemicals, like resveratrol (res), offer potential but have poor water solubility, limiting use.
- Novel delivery systems are needed for hydrophobic therapeutic agents.
Purpose of the Study:
- To develop and characterize a novel nanoparticle for delivering resveratrol (res).
- To evaluate the efficacy and selectivity of res-loaded nanoparticles in breast cancer cells.
- To explore the potential of these nanoparticles for breast cancer diagnosis and therapy.
Main Methods:
- Resveratrol (res)-loaded nanoparticles synthesized using Pluronic F127 and Vitamin E-TPGS via emulsion method.
- Nanoparticle characterization included SEM, tunable resistive pulse sensing, EE%, and DL%.
- Cellular uptake and viability assays (flow cytometry, MTT) performed on breast cancer and control cell lines.
Main Results:
- Spherical res-loaded nanoparticles produced, size 179±22 nm, with high encapsulation efficiency (73±0.9%) and drug loading (6.2±0.1%).
- Nanoparticles exhibited higher uptake in breast cancer cells (MCF-7, MDA-MB-231) than control (MCF-10A).
- Res-loaded nanoparticles significantly reduced breast cancer cell viability without affecting control cells.
Conclusions:
- The synthesized nanoparticle effectively encapsulates hydrophobic drugs like resveratrol.
- The nanoparticle demonstrates high efficacy and selectivity against breast cancer cells.
- This nanoparticle system is a promising candidate for the diagnosis and therapy of breast cancer.

