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E-selectin targeted immunoliposomes for rapamycin delivery to activated endothelial cells
Shima Gholizadeh1, Ganesh Ram R Visweswaran2, Gert Storm1
1Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, Utrecht, The Netherlands.
International Journal of Pharmaceutics
|October 18, 2017
Summary
Targeted immunoliposomes deliver rapamycin to inflamed endothelial cells, inhibiting their proliferation and inflammatory responses. This approach offers a promising strategy for treating inflammatory disorders by specifically targeting activated cells.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Immunology
Background:
- Activated endothelial cells are central to inflammatory disorders.
- Rapamycin (mammalian target of rapamycin, mTOR) is an inhibitor of inflammatory signaling.
- Targeted drug delivery can enhance therapeutic efficacy and reduce side effects.
Purpose of the Study:
- To develop anti-E-selectin immunoliposomes for targeted delivery of rapamycin.
- To investigate the efficacy of these immunoliposomes in inhibiting activated endothelial cells.
Main Methods:
- Liposomes were formulated with DPPC, Cholesterol, and DSPE-PEG-Mal.
- Rapamycin was loaded into liposomes via lipid film hydration.
- Immunoliposomes were functionalized with anti-E-selectin antibodies.
- Cell binding assays were performed on TNF-α activated endothelial cells.
Main Results:
- Immunoliposomes specifically bound to TNF-α activated endothelial cells.
- Internalized rapamycin-loaded immunoliposomes inhibited endothelial cell proliferation and migration.
- Expression of inflammatory mediators was reduced by the immunoliposomes.
Conclusions:
- Rapamycin-loaded immunoliposomes demonstrate specific targeting of inflamed endothelial cells.
- This targeted delivery system effectively inhibits key aspects of endothelial cell-mediated inflammation.
- The findings support the potential of this nanomedicine approach for inflammatory disease treatment.