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Formulation and Evaluation of Morin-Loaded Solid Lipid Nanoparticles.
Yuri Ikeuchi-Takahashi1, Chizuko Ishihara, Hiraku Onishi
1Department of Drug Delivery Research, Hoshi University.
Biological & Pharmaceutical Bulletin
|June 21, 2016
Summary
This study optimized solid lipid nanoparticles (SLNs) using specific polyvinyl alcohols (PVA) and ethylcellulose (EC). Optimized SLNs enhanced morin bioavailability through sustained release and improved intestinal permeation, increasing Cmax and AUC0-360.
Area of Science:
- Pharmaceutical Sciences
- Nanotechnology
- Drug Delivery Systems
Background:
- Solid lipid nanoparticles (SLNs) are a promising drug delivery system.
- The formulation of SLNs, particularly the choice of surfactants and polymers, significantly impacts their properties.
- Polyvinyl alcohols (PVAs) with varying degrees of saponification and polymerization are used in SLN preparation.
Purpose of the Study:
- To investigate the effect of different polyvinyl alcohols (PVAs) and the presence of ethylcellulose (EC) on solid lipid nanoparticle (SLN) formation and morin release.
- To optimize SLN formulations for enhanced bioavailability of encapsulated morin.
- To evaluate the impact of particle size and sustained release properties on pharmacokinetic parameters.
Main Methods:
- Preparation of solid lipid nanoparticle (SLN) suspensions using hard fat, ethylcellulose (EC), polyvinyl alcohols (PVAs), and polysorbate 60.
- Characterization of SLNs, including particle size analysis.
- In vitro release studies of morin from SLNs.
- In vivo pharmacokinetic studies to determine Cmax and AUC0-360 of morin.
Main Results:
- Different saponification degrees of PVA were required for SLN formation with or without EC.
- SLNs formulated with EC exhibited more sustained morin release compared to those without EC.
- Optimized SLNs with EC and a very low-saponification-degree PVA showed reduced particle size, leading to higher Cmax and AUC0-360, indicating improved bioavailability.
Conclusions:
- The selection of appropriate PVA is crucial for reproducible SLN formation, with low-saponification PVA for EC-free systems and high-saponification PVA for EC-containing systems.
- Ethylcellulose incorporation and optimized PVA selection enhance morin's sustained release and bioavailability.
- Optimized SLNs with EC and very low-saponification PVA represent an effective strategy for improving oral drug delivery by enhancing enterocyte accessibility and intestinal permeation.
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