Bioactive Molecules Research Laboratory, Doctoral School of Sciences and Technologies, Faculty of Sciences, Lebanese University, Jdeidet El-Metn 90656, Lebanon.
UMR-5280, CNRS-University Lyon-1, 5 rue de la Doua, 69100 Villeurbanne, France.
Molecules. 2021 Nov 12;26(22):6840. doi: 10.3390/molecules26226840.
The essential oil component α-pinene has multiple biological activities. However, its application is limited owing to its volatility, low aqueous solubility, and chemical instability. For the aim of improving its physicochemical properties, α-pinene was encapsulated in conventional liposomes (CLs) and drug-in-cyclodextrin-in-liposomes (DCLs). Hydroxypropyl-β-cyclodextrin/α-pinene (HP-β-CD/α-pinene) inclusion complexes were prepared in aqueous solution, and the optimal solubilization of α-pinene occurred at HP-β-CD:α-pinene molar ratio of 7.5:1. The ethanol-injection method was applied to produce different formulations using saturated (Phospholipon 90H) or unsaturated (Lipoid S100) phospholipids in combination with cholesterol. The size, the phospholipid and cholesterol incorporation rates, the encapsulation efficiency (EE), and the loading rate (LR) of α-pinene were determined, and the storage stability of liposomes was assessed. The results showed that α-pinene was efficiently entrapped in CLs and DCLs with high EE values. Moreover, Lipoid S100 CLs displayed the highest LR (22.9 ± 2.2%) of α-pinene compared to the other formulations. Both carrier systems HP-β-CD/α-pinene inclusion complex and Lipoid S100 CLs presented a gradual release of α-pinene. Furthermore, the DPPH radical scavenging activity of α-pinene was maintained upon encapsulation in Lipoid S100 CLs. Finally, it was found that all formulations were stable after three months of storage at 4 °C.
α-蒎烯是一种具有多种生物活性的精油成分。然而，由于其挥发性、低水溶性和化学不稳定性，其应用受到限制。为了改善其物理化学性质，将 α-蒎烯包封在常规脂质体（CL）和药物-环糊精-脂质体（DCL）中。在水溶液中制备了羟丙基-β-环糊精/α-蒎烯（HP-β-CD/α-蒎烯）包合物，在 HP-β-CD：α-蒎烯摩尔比为 7.5:1 时，α-蒎烯的溶解度最佳。采用乙醇注入法，用饱和（Phospholipon 90H）或不饱和（Lipoid S100）磷脂与胆固醇结合，制备不同配方。测定了脂质体的粒径、磷脂和胆固醇包封率、包封效率（EE）和载药量（LR），并评估了脂质体的储存稳定性。结果表明，α-蒎烯在 CL 和 DCL 中被有效包封，EE 值较高。此外，与其他配方相比，Lipoid S100 CL 显示出最高的 α-蒎烯 LR（22.9±2.2%）。两种载体系统 HP-β-CD/α-蒎烯包合物和 Lipoid S100 CL 都表现出α-蒎烯的逐渐释放。此外，α-蒎烯的 DPPH 自由基清除活性在包封于 Lipoid S100 CL 中时得以保持。最后，发现所有配方在 4°C 下储存三个月后均稳定。
