New findings on the incorporation of essential oil components into liposomes composed of lipoid S100 and cholesterol

• DOI: 10.1016/j.ijpharm.2019.02.022
• Publication Date: 2019-03-02T22:54:57Z
• Authors: Zahraa Hammoud; Riham Gharib; Sophie Fourmentin; Abdelhamid Elaissari; Hélène Greige-Gerges
• Keywords: liposomes; henry constant; 04 agricultural and veterinary sciences; [SDV.SP]Life Sciences [q-bio]/Pharmaceutical sciences; 16. Peace & justice; release; [SDV.SP] Life Sciences [q-bio]/Pharmaceutical sciences; Drug Liberation; Cholesterol; 0404 agricultural biotechnology; Drug Stability; Solubility; aqueous solubility; Liposomes; Oils, Volatile; Phosphatidylcholines; encapsulation; essential oil components

The encapsulation of essential oil components into liposomes was demonstrated to improve their solubility and chemical stability. In this study, we investigated the effect of chemical structure, Henry's law constant (Hc), and aqueous solubility of essential oil components on their liposomal encapsulation. Estragole, eucalyptol, isoeugenol, pulegone, terpineol, and thymol were encapsulated in lipoid S100-liposomes using the ethanol injection method. The Hc values were determined. The incorporation in liposomes was more efficient (encapsulation efficiency > 90%) for the essential oil components exhibiting low aqueous solubility (estragole, isoeugenol, and pulegone). Moreover, efficient entrapment into vesicles (loading rate > 18%) was obtained for isoeugenol, terpineol, and thymol. This result suggests that the presence of a hydroxyl group in the structure and a low Hc value enhance the entrapment of essential oil components into liposomes. Furthermore, drug release rate from liposomes was controlled by the loading rate of essential oil components into liposomes, the size of particles, the location of essential oil components within the lipid bilayer, and the cholesterol incorporation rate of liposomes. Finally, considerable concentrations of isoeugenol, pulegone, terpineol, and thymol were retained in liposomes after 10 months with respect to the initial concentration.