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Updated: May 30, 2026
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Multi-color Localization Microscopy of Single Membrane Proteins in Organelles of Live Mammalian Cells
Published on: June 30, 2018
Effect of integrin targeting and PEG shielding on polyplex micelle internalization studied by live-cell imaging
F M Mickler1, Y Vachutinsky, M Oba
1Department of Chemistry and Biochemistry and Center for NanoScience, Ludwig-Maximilians-Universität München, Butenandtstr. 5-13, D-81377 München, Germany.
Summary
Targeting cancer with RGD-equipped micelles enhances cellular uptake and gene expression. Higher PEG shielding improves specificity for integrin-targeted micelles, making them promising for cancer therapy.
Area of Science:
- Biotechnology
- Nanomedicine
- Cancer Therapy
Background:
- Integrins α(v)β(3) and α(v)β(5) are crucial for tumor growth and metastasis.
- Targeting these integrins offers a promising strategy for cancer treatment.
- Polyplex micelles with cyclic RGD peptides can target specific integrins.
Purpose of the Study:
- To investigate the impact of RGD ligand on micelle endocytosis.
- To evaluate the influence of PEG shielding on micelle targeting specificity and internalization.
- To compare the efficacy of different micelle formulations for gene delivery.
Main Methods:
- Utilized fluorescently labeled, targeted, and untargeted micelles.
- Conducted live-cell imaging with fluorescence microscopy and flow cytometry.
- Compared two micelle types with different PEG shell layers (PEG12 and PEG17).
Main Results:
- RGD ligand accelerated micelle internalization into integrin-expressing cells via clathrin-mediated endocytosis.
- Higher PEG shielding (PEG17) enhanced specific endocytosis of integrin-targeted micelles.
- PEG17 RGD(+) micelles demonstrated superior reporter gene expression and efficacy at lower doses.
Conclusions:
- RGD-functionalized micelles show enhanced cellular uptake and specific targeting of integrins.
- PEG shielding significantly influences the specificity and efficiency of micelle-mediated gene delivery.
- PEG17 shielded micelles with RGD ligands are a promising candidate for clinical cancer gene therapy.
