Abstract

The encapsulation of bicyclic monoterpene α-pinene into solid lipid nanoparticles (SLN) is reported using experimental factorial design, followed by high-end dispersion analyzer LUMiSizer®. This equipment allows the characterization of the α-pinene-loaded SLN instability phenomena (e.g., sedimentation, flotation or coagulation), as well as the determination of the velocity distribution in the centrifugal field and the particle size distribution. In this work, SLN were produced by hot high-pressure homogenization technique. The influence of the independent variables, surfactant and lipid ratio on the physicochemical properties of SLN, such as mean particle size (Z-Ave), polydispersity index (PDI) and zeta potential (ZP), was estimated using a 22-factorial design. The Z-Ave and PDI were analyzed by dynamic light scattering, while ZP measurements were recorded by electrophoretic light scattering. Based on the obtained results, the optimal SLN dispersion was composed of 1 wt.% of α-pinene, 4 wt.% of solid lipid (Imwitor® 900 K) and 2.5 wt.% of surfactant (Poloxamer 188), depicting 136.7 nm of Z-Ave, 0.170 of PDI and 0 mV of ZP. Furthermore, LUMISizer® has been successfully used in the stability analysis of α-pinene-loaded SLN.

Highlights

  • Innovative, non-toxic lipid nanoparticles, such as solid lipid nanoparticles (SLN), are recognized as suitable delivery carriers for lipophilic active pharmaceutical ingredients (APIs) [1,2]

  • As main shortcoming of experimental design is to deal with increasing number of factors and/or levels, in this work 22 full factorial design was developed in order to optimize α-pinene-loaded SLN

  • The main purpose of the experimental factorial design was the analysis of the effects for different factors with the simultaneously determination of the factors’ interaction

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Summary

Introduction

Innovative, non-toxic lipid nanoparticles, such as solid lipid nanoparticles (SLN), are recognized as suitable delivery carriers for lipophilic active pharmaceutical ingredients (APIs) [1,2]. Alpha-pinene is a colorless liquid at room temperature, substantially temperature, substantially insoluble in water, being a suitable candidate for the loading in insoluble in water, being a suitable candidate for the loading in lipid nanoparticles as SLN for lipid nanoparticles as SLN for modified release. This monoterpene can be widely used as a raw modified release.

Material and Methods
Lipid Screening
Experimental Factorial Design
Preparation of Nanoparticles
Characterization of Nanoparticles
Accelerated Stability Analysis
Design
Stability Analysis with LUMiSizer
Results are in Table and
Conclusions
Full Text
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