Abstract
Lipid nanoparticles based on multiple emulsion (W/O/W) systems are suitable for incorporating hydrophilic active substances, including iridoid glycosides. This study involved optimization of composition of lipid nanoparticles, incorporation of active compounds (aucubin and catalpol), evaluation of stability of the resulting nanocarriers, and characterization of their lipid matrix. Based on 32 factorial design, an optimized dispersion of lipid nanoparticles (solid lipid:surfactant—4.5:1.0 wt.%) was developed, predisposed for the incorporation of iridoid glycosides by emulsification-sonication method. The encapsulation efficiency of the active substances was determined at nearly 90% (aucubin) and 77% (catalpol). Regarding the stability study, room temperature was found to be the most suitable for maintaining the expected physicochemical parameter values (particle size < 100 nm; polydispersity index < 0.3; zeta potential > |± 30 mV|). Characterization of the lipid matrix confirmed the nanometer size range of the resulting carriers (below 100 nm), as well as the presence of the lipid in the stable β’ form.
Highlights
The choice of the method of the synthesis of lipid nanoparticles is determined by the nature of the active substance to be incorporated, the target structure and size of the carrier, and the expected release profile of the encapsulated active ingredient, which is closely related to the intended application site [1,2]
The measured data obtained by determining the values of the dependent variables for all prepared samples of the lipid nanoparticle dispersions are listed in Table 1 and analyzed statistically with the help of Statistica
The essence of optimizing the composition of lipid nanoparticles is the possibility to produce dispersions that are suitable for the incorporation of the planned active compounds and stable under various temperature conditions for a specified period of time
Summary
The choice of the method of the synthesis of lipid nanoparticles is determined by the nature of the active substance to be incorporated, the target structure and size of the carrier, and the expected release profile of the encapsulated active ingredient, which is closely related to the intended application site [1,2]. The level of encapsulation efficiency achieved in dispersions of lipid nanoparticles containing substances of hydrophilic nature typically does not exceed 80% [3,4,5]. In this case, the recommended method is based on a multiple emulsion (W/O/W), which enables the incorporation of hydrophilic active substances and the formation of lipid nanoparticles with a size below 100 nm. The method consists in dissolving the active compound in the aqueous phase of the internal W/O emulsion formed as a result of intensive mixing and homogenization by means of a high-speed homogenizer. The method requires high accuracy in terms of maintaining appropriate temperatures at subsequent process steps, as the dispersions of lipid nanoparticles obtained by applying this method display a trend for a relatively high polydispersity index [4,6]
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