Bioactive Molecules Research Laboratory, Doctoral School of Sciences and Technologies, Faculty of Sciences, Section II, Lebanese University, Lebanon; University Claude Bernard Lyon-1, CNRS, LAGEP-UMR 5007, F-69622 Lyon, France.
Bioactive Molecules Research Laboratory, Doctoral School of Sciences and Technologies, Faculty of Sciences, Section II, Lebanese University, Lebanon.
Int J Pharm. 2019 Apr 20;561:161-170. doi: 10.1016/j.ijpharm.2019.02.022. Epub 2019 Mar 2.
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 (H), 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 H 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.
将精油成分包封到脂质体中被证明可以提高其溶解度和化学稳定性。在这项研究中,我们研究了精油成分的化学结构、亨利定律常数(H)和水溶解度对其脂质体包封的影响。采用乙醇注入法将茴香脑、桉油醇、异丁香酚、黄樟素、萜品醇和百里香酚包封在脂质体 S100 中。测定了 H 值。对于表现出低水溶性的精油成分(茴香脑、异丁香酚和黄樟素),包封入脂质体中的效率更高(包封效率>90%)。此外,异丁香酚、萜品醇和百里香酚的有效包封率(载药量>18%)。这一结果表明,结构中存在羟基和低 Hc 值有助于将精油成分有效包封入脂质体中。此外,脂质体中精油成分的载药量、颗粒大小、精油成分在脂质双层中的位置以及脂质体中胆固醇的掺入率控制着药物从脂质体中的释放速率。最后,与初始浓度相比,异丁香酚、黄樟素、萜品醇和百里香酚在脂质体中的保留浓度在 10 个月后仍相当可观。