Microencapsulation of nanoemulsions: novel Trojan particles for bioactive lipid molecule delivery

Xiang Li¹, Nicolas Anton¹, Thi Minh Chau Ta¹, Minjie Zhao², Nadia Messaddeq³, Thierry F Vandamme^1
1University of Strasbourg, Faculty of Pharmacy, UMR CNRS 7199 Laboratory of Conception and Application of Bioactive Molecules (Biogalenic Pharmacy team); ²University of Strasbourg, Faculty of Pharmacy, CNRS UMR 7178, IPHC, Laboratory of Analytic Chemistry and Food Science; ³Institute of Genetics and Molecular and Cellular Biology (IGBMC), UMR University of Strasbourg/CNRS/INSERM/Collège de France, Illkirch, France

Background: Nanoemulsions consist of very stable nanodroplets of oil dispersed in an aqueous phase, typically below 300 nm in size. They can be used to obtain a very fine, homogeneous dispersion of lipophilic compounds in water, thus facilitating their handling and use in nanomedicine. However, the drawback is that they are suspended in an aqueous media. This study proposes a novel technique for drying lipid nanoemulsion suspensions to create so-called Trojan particles, ie, polymer microparticles (around 2 µm) which very homogeneously “entrap” the nano-oil droplets (around 150 nm) in their core.
Methods: Microencapsulation of the nanoemulsions was performed using a spray-drying process and resulted in a dried powder of microparticles. By using a low-energy nanoemulsification method and relatively gentle spray-drying, the process was well suited to sensitive molecules. The model lipophilic molecule tested was vitamin E acetate, encapsulated at around 20% in dried powder.
Results: We showed that the presence of nanoemulsions in solution before spray-drying had a significant impact on microparticle size, distribution, and morphology. However, the process itself did not destroy the oil nanodroplets, which could easily be redispersed when the powder was put back in contact with water. High-performance liquid chromatography follow-up of the integrity of the vitamin E acetate showed that the molecules were intact throughout the process, as well as when conserved in their dried form.
Conclusion: This study proposes a novel technique using a spray-drying process to microencapsulate nanoemulsions. The multiscale object formed, so-called Trojan microparticles, were shown to successfully encapsulate, protect, and release the lipid nanodroplets.

Keywords: nanoemulsions, microparticles, Trojan particle, spray-drying, low-energy emulsification, vitamin E acetate