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Endothelial Cell Targeting by cRGD-Functionalized Polymeric Nanoparticles under Static and Flow Conditions
Lucía Martínez-Jothar1, Arjan D Barendrecht2, Anko M de Graaff3
1Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, Universiteitsweg 99, 3584 CG Utrecht, The Netherlands.
Nanomaterials (Basel, Switzerland)
|July 16, 2020
Summary
Cyclic-RGD peptide-functionalized nanoparticles target angiogenic endothelium by binding to αvβ3 integrin. Red blood cells enhance nanoparticle association with endothelial cells under flow, aiding in vivo prediction.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Drug Delivery
Background:
- αvβ3 integrin is crucial for angiogenesis in tumors.
- RGD peptide-functionalized nanocarriers target αvβ3-overexpressing tumor neovasculature.
- Poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) are suitable drug delivery vehicles.
Purpose of the Study:
- Evaluate PEGylated PLGA NPs functionalized with cyclic-RGD (cRGD) for targeting angiogenic endothelium.
- Investigate the effect of cRGD surface density on NP-endothelial cell interactions.
- Assess NP-cell interactions under static and dynamic (flow) conditions, including the role of red blood cells (RBCs).
Main Methods:
- Preparation of cRGD-functionalized PLGA NPs (~300 nm) using maleimide-thiol chemistry.
- Evaluation of NP-human umbilical vein endothelial cell (HUVEC) interactions via flow cytometry and microscopy.
- Assessment of NP-HUVEC interactions under static and flow conditions, with and without added RBCs.
Main Results:
- cRGD-NP cell association was dependent on time, concentration, and cRGD density under static conditions.
- NP-HUVEC interactions under flow were also time- and cRGD density-dependent.
- The presence of RBCs increased NP association with HUVECs by 3 to 8-fold under flow conditions.
Conclusions:
- cRGD-functionalized NPs effectively target angiogenic endothelium.
- Simulating in vivo conditions with flow and RBCs provides a more accurate prediction of nanocarrier behavior.
- This model system aids in developing and screening novel endothelium-targeted nanocarriers for drug delivery.
