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Preparation, Administration, and Assessment of In Vivo Tissue-Specific Cellular Uptake of Fluorescent Dye-Labeled Liposomes
Published on: July 30, 2020
Fluorescent probe-labeled lipid microsphere uptake by human endothelial cells: a flow cytometric study
K Suzuki1, K Takahashi, Y Matsuki
1Internal Medicine I, National Defense Medical College, Saitama, Japan.
Japanese Journal of Pharmacology
|December 1, 1992
Summary
Lipid microspheres show preferential uptake by endothelial cells, crucial for targeted drug delivery in vascular diseases. This selective accumulation enhances the efficacy of lipid-based drug carriers in vivo.
Area of Science:
- Biomedical Engineering
- Drug Delivery Systems
- Cell Biology
Background:
- Lipid microspheres are established drug carriers, notably for prostaglandin E1 (lipo-PGE1) in treating chronic arterial occlusive diseases.
- Lipo-PGE1 exhibits superior in vivo activity compared to free prostaglandin E1, highlighting the potential of lipid-based formulations.
Purpose of the Study:
- To investigate the preferential uptake of lipid microspheres by endothelial cells.
- To validate lipid microspheres as targeted drug carriers for vascular applications.
Main Methods:
- Lipid microspheres were labeled with a stable fluorescent probe, DiI (DiI-LM).
- Cellular uptake of DiI-LM was quantified using flow cytometry in various cell types, including endothelial cells, fibroblasts, and neutrophils.
- Fluorescence microscopy was employed to visualize DiI-LM localization within cells.
Main Results:
- Endothelial cells (human umbilical vein and ECV304 cell line) demonstrated high uptake of DiI-LM (81% and 61%, respectively).
- Non-endothelial cells (fibroblasts, 3T3 cells, neutrophils) showed significantly lower uptake (<7%).
- Prominent perinuclear fluorescence was observed in endothelial cells, suggesting specific intracellular accumulation.
Conclusions:
- Lipid microspheres are selectively internalized by endothelial cells.
- DiI-LM and flow cytometry are valuable tools for studying the mechanism of selective lipid microsphere accumulation in vascular walls.
- These findings support the use of lipid microspheres for targeted endothelial drug delivery.

