Department of Drug and Health Sciences, University of Catania, Viale Andrea Doria 6, 95125 Catania, Italy.
Department of Chemical Sciences, University of Catania, Viale Andrea Doria 6, 95125 Catania, Italy.
Molecules. 2021 Aug 13;26(16):4903. doi: 10.3390/molecules26164903.
Glycyrrhetic acid (GA) and stearyl glycyrrhetinate (SG) are two interesting compounds from , showing numerous biological properties widely applied in the pharmaceutical and cosmetic fields. Despite these appreciable benefits, their potential therapeutic properties are strongly compromised due to unfavourable physical-chemical features. The strategy exploited in the present work was to develop solid lipid nanoparticles (SLNs) as carrier systems for GA and SG delivery. Both formulations loaded with GA and SG (GA-SLNs and SG-SLNs, respectively) were prepared by the high shear homogenization coupled to ultrasound (HSH-US) method, and we obtained good technological parameters. DSC was used to evaluate their thermotropic behaviour and ability to act as carriers for GA and SG. The study was conducted by means of a biomembrane model (multilamellar vesicles; MLVs) that simulated the interaction of the carriers with the cellular membrane. Unloaded and loaded SLNs were incubated with the biomembranes, and their interactions were evaluated over time through variations in their calorimetric curves. The results of these studies indicated that GA and SG interact differently with MLVs and SLNs; the interactions of SG-SLNs and GA-SLNs with the biomembrane model showed different variations of the MLVs calorimetric curve and suggest the potential use of SLNs as delivery systems for GA.
甘草次酸(GA)和硬脂基甘草亭酸(SG)是 中的两种有趣化合物,具有多种生物特性,广泛应用于制药和化妆品领域。尽管它们具有这些显著的益处,但由于物理化学性质不佳,其潜在的治疗特性受到了严重影响。本工作中采用的策略是开发固体脂质纳米粒(SLN)作为 GA 和 SG 传递的载体系统。通过高剪切匀化与超声(HSH-US)联合方法制备载有 GA 和 SG 的两种制剂(分别为 GA-SLNs 和 SG-SLNs),并获得了良好的工艺参数。通过差示扫描量热法(DSC)评估它们的热行为以及作为 GA 和 SG 载体的能力。通过模拟载体与细胞膜相互作用的生物膜模型(多层囊泡;MLVs)进行了研究。将未加载和加载的 SLN 与生物膜孵育,并通过其热谱曲线的变化随时间评估它们的相互作用。这些研究的结果表明,GA 和 SG 与 MLVs 和 SLNs 的相互作用方式不同;SG-SLNs 和 GA-SLNs 与生物膜模型的相互作用显示出 MLVs 热谱曲线的不同变化,表明 SLN 有潜力作为 GA 的递送系统。