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Pore size effect on adsorption and release of metoprolol tartrate in mesoporous silica: Experimental and molecular
Shicheng Luo1, Jiakang Hao1, Yanmei Gao1
1State Key Laboratory of Organic-Inorganic Composites, Beijing University of Chemical Technology, Beijing 100029, PR China.
Abstract:
Mesoporous silica nanoparticles (MSNs) have been widely studied as drug carriers to get sustained release behaviors, however, their application in sustained release of metoprolol tartrate (MPT) is limited. The possible reason is due to MPT molecule being bulky, while normal type MSNs like MCM-41 and SBA-15 have pore sizes of only 3-6 nm. In this study, two MCF-26 type MSNs were prepared with pore size of 11 or 15 nm, and used to conduct MPT release in comparison with MCM-41 and SBA-15. Both molecular simulation and MPT release experiments were performed to identify the pore size effect on adsorption and diffusion (release) of MPT in these MSNs. Finally, a kind of pH-sensitive MPT drug delivery system was obtained by coating the chosen MCF-26@MPT with an enteric polymer, which might find promising application in treating morning hypertension attack by orally administrating the drug delivery system before bedtime.
Insights
Mesoporous silica nanoparticles with larger pores effectively carry metoprolol tartrate for sustained release. A pH-sensitive system was developed for potential morning hypertension treatment.
Area of Science:
- Materials Science
- Nanotechnology
- Pharmaceutical Sciences
Background:
- Mesoporous silica nanoparticles (MSNs) are explored for sustained drug delivery.
- Metoprolol tartrate (MPT) delivery is limited by bulky molecules and small MSN pores (3-6 nm).
Purpose of the Study:
- To investigate the effect of MSN pore size on metoprolol tartrate (MPT) adsorption and release.
- To develop a pH-sensitive MPT drug delivery system for potential hypertension treatment.
Main Methods:
- Synthesized two types of MCF-26 mesoporous silica nanoparticles with pore sizes of 11 nm and 15 nm.
- Compared MPT release from MCF-26, MCM-41, and SBA-15 MSNs using molecular simulation and experimental release studies.
- Coated MPT-loaded MCF-26 nanoparticles with an enteric polymer to create a pH-sensitive system.
Main Results:
- Larger pore sizes (11-15 nm) in MCF-26 MSNs improved MPT adsorption and sustained release compared to MCM-41 and SBA-15.
- Molecular simulations and release experiments confirmed the pore size effect on MPT diffusion.
- A functional pH-sensitive drug delivery system was successfully fabricated.
Conclusions:
- MCF-26 MSNs with optimized pore sizes are suitable carriers for metoprolol tartrate sustained release.
- The developed pH-sensitive system shows promise for managing morning hypertension attacks via oral administration before sleep.
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