Lipid Nanoparticles Loaded with Iridoid Glycosides: Development and Optimization Using Experimental Factorial Design
Marta Dąbrowska1,2, Eliana B Souto2,3, Izabela Nowak1
1Department of Applied Chemistry, Faculty of Chemistry, Adam Mickiewicz University in Poznań, Uniwersytetu Poznańskiego 8, 61-614 Poznan, Poland.
Molecules (Basel, Switzerland)
|June 2, 2021
Summary
Optimized lipid nanoparticles effectively encapsulate hydrophilic iridoid glycosides like aucubin and catalpol. These nanocarriers demonstrate excellent stability at room temperature, maintaining optimal particle size and charge for potential therapeutic applications.
Area of Science:
- Pharmaceutical Nanotechnology
- Drug Delivery Systems
- Biochemistry
Background:
- Multiple emulsion (W/O/W) systems are effective for encapsulating hydrophilic compounds.
- Iridoid glycosides possess therapeutic potential but require suitable delivery systems.
- Lipid nanoparticles offer a promising platform for enhanced drug delivery.
Purpose of the Study:
- To optimize the composition of lipid nanoparticles for iridoid glycoside incorporation.
- To evaluate the stability and physicochemical properties of the developed nanocarriers.
- To characterize the lipid matrix of the nanocarriers.
Main Methods:
- Utilized a 3^2 factorial design for optimization of lipid nanoparticle composition (solid lipid:surfactant ratio).
- Emulsification-sonication method for incorporating aucubin and catalpol into W/O/W lipid nanoparticles.
- Stability studies under various conditions, particle size analysis, polydispersity index, zeta potential measurements, and lipid matrix characterization (X-ray diffraction).
Main Results:
- An optimized lipid nanoparticle dispersion (4.5:1.0 wt.% solid lipid:surfactant) was developed.
- High encapsulation efficiencies achieved: ~90% for aucubin and ~77% for catalpol.
- Optimal stability observed at room temperature, with particle size < 100 nm, PDI < 0.3, and zeta potential > |± 30 mV|.
- Lipid matrix characterization confirmed nanometer-sized carriers and the stable β' polymorphic form.
Conclusions:
- Optimized W/O/W lipid nanoparticles are suitable for efficient encapsulation of hydrophilic iridoid glycosides.
- The developed nanocarriers exhibit good stability at room temperature, preserving key physicochemical properties.
- The findings support the potential of these lipid nanoparticles for delivering iridoid glycosides in pharmaceutical applications.
