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Updated: Jun 24, 2026
09:34
Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells
Published on: February 9, 2019
Nanoparticle processing in the solid state dramatically increases the cell membrane permeation of a
Toshiro Fukami1, Tatsuya Ishii, Takeshi Io
1College of Pharmacy, Nihon University, Chiba 274-8555, Japan. fukami.toshiro@nihon-u.ac.jp
Molecular Pharmaceutics
|March 14, 2009
Summary
This study introduces a novel nanoparticle method to enhance the solubility and cell membrane permeability of probucol, a drug used to lower high cholesterol levels and reduce coronary heart disease risk.
Area of Science:
- Pharmaceutical Science
- Materials Science
- Biomedical Engineering
Background:
- High cholesterol (hypercholesterolemia) is a significant risk factor for coronary heart diseases.
- Probucol is an effective cholesterol-lowering drug but suffers from very low aqueous solubility (5 ng/mL).
- Poor solubility limits probucol's bioavailability and therapeutic efficacy.
Purpose of the Study:
- To develop a novel method for increasing probucol's solubility and cell membrane permeability.
- To enhance the overall efficiency of probucol as a cholesterol-reducing agent.
Main Methods:
- A new nanoparticle formulation process involving grinding probucol with sodium dodecylsulfate and a methacrylic copolymer.
- Solid-state Nuclear Magnetic Resonance (NMR) spectroscopy to analyze drug-excipient interactions and physical state.
Main Results:
- The grinding process successfully converted crystalline probucol to an amorphous state.
- Nanoparticle formation was achieved, indicating probucol's proximity to the copolymer.
- The novel method significantly increased probucol's aqueous solubility and cell membrane permeability.
Conclusions:
- The developed nanoparticle formulation effectively enhances probucol solubility and bioavailability.
- This approach offers a promising strategy for improving the delivery and efficacy of poorly soluble drugs like probucol.
- Further research can explore this method for other hydrophobic therapeutic agents.
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