Objectives: Resveratrol (Res) was a naturally occurring polyphenol compound. It has various beneficial effects, including anti-inflammatory, anti-oxidant and anti-cancer effects. However, the anti-cancer activity was hindered by its low targeting and drug release performance. Thus, we synthesized transferrin-cathepsin B cleavable peptide modified mesoporous silica nanoparticle encapsulated Res (Tf-Res-MSN).
Methods: Res was encapsulated in mesoporous silica nanoparticles (MSN), which was a kind of drug carrier complex. Tf was modified to recognize the cancer cells. Cathepsin B cleavable peptide (Pep) was used to combine Res-MSN complex and Tf to construct the final product. Pep was used as linker and trigger for Res release.
Key findings: The smart nanocarriers were increased the drug release performance of Res in human breast cancer (MCF-7) cells. The physicochemical properties of Tf-Res-MSN were assessed by zeta potential, UV-Prove, diffraction scanning calorimetry (DSC), nitrogen physisorption analysis and transmission electron microscope (TEM). MTT assay, AO and Annexin V-FITC/PI staining were performed to explore the anti-tumour activity of Tf-Res-MSN. The results showed that Tf-Res-MSN significantly decreased cell viability and increased cell apoptosis. The inhibition rate and apoptotic rate of Tf-Res-MSN in MCF-7 cells were 95.75% and 80.8%, respectively.
Conclusion: Our study demonstrated that Tf-Res-MSN was a valuable technique with potential value in breast cancer applications.
Keywords: breast cancer; mesoporous silica; resveratrol; transferrin.
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