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Surface-functionalized layered double hydroxide nanocontainers as bile acid sequestrants for lowering hyperlipidemia
Chiao-Wen Lin1, Shi-Xiang Lin1, Ranjith Kumar Kankala2
1Department of Life Science, National Dong Hwa University, Hualien 97401, Taiwan.
International Journal of Pharmaceutics
|October 7, 2020
Summary
Surface-functionalized layered double hydroxides (LDHs) were developed as bile acid sequestrants. These modified nanoplates effectively reduced cholesterol in mice, demonstrating high biocompatibility for potential medical applications.
Area of Science:
- Materials Science
- Biomedical Engineering
- Nanotechnology
Background:
- Surface modification of nanomaterials enhances their properties for medical applications.
- Layered double hydroxides (LDHs) are versatile 2D nanocontainers with potential therapeutic uses.
Purpose of the Study:
- To fabricate surface-functionalized LDHs for use as intestinal bile acid sequestrants.
- To evaluate the in vitro and in vivo efficacy and biocompatibility of these modified LDHs.
Main Methods:
- LDHs were modified with N1-(3-trimethoxysilylpropyl) diethylenetriamine (LDHs-N3) and further functionalized with ethylene diamine.
- An enteric co-polymer was used to coat the modified LDHs for stability in acidic environments.
- In vitro bile acid adsorption and in vivo cholesterol reduction studies in mice were performed.
Main Results:
- Surface-functionalized LDHs demonstrated significant in vitro cholic acid adsorption capacity.
- Enteric polymer-coated LDHs reduced cholesterol by 8.2% in high-fat diet-fed mice.
- Histology and organ weight analysis confirmed the high in vivo biocompatibility of the modified LDHs.
Conclusions:
- Surface-functionalized 2D nanoplates show great potential as effective intestinal bile acid sequestrants.
- The developed LDHs offer a promising strategy for managing cholesterol levels and related conditions.
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