Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Via Aldo Moro 2, Siena 53100, Italy; Centre for Colloid and Surface Science (CSGI), University of Florence, Via della Lastruccia 3, Sesto Fiorentino, FI 50019, Italy.
Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Via Aldo Moro 2, Siena 53100, Italy; Centre for Colloid and Surface Science (CSGI), University of Florence, Via della Lastruccia 3, Sesto Fiorentino, FI 50019, Italy.
Biophys Chem. 2019 Mar;246:25-34. doi: 10.1016/j.bpc.2019.01.002. Epub 2019 Jan 14.
Tyrosol, hydroxytyrosol and oleuropein are among the major phenolic compounds in fruits, leaves and oils from Olea europaea L. These natural antioxidants molecules revealed several beneficial effects on human health, but a low bioavailability and accessibility to targeted site. Liposomes are drug/nutraceutical delivery carriers, used for driving bioactive molecules to desired target tissues, decreasing potential side effects and protecting the encapsulated molecule from enzymatic metabolic processes. In this study, zwitterionic liposomes containing tyrosol, hydroxytyrosol and oleuropein were synthesized and characterized for their size and surface charge. Particular attention was devoted to the determination of encapsulation efficiency (EE%), quantifying the loaded Tyr, HTyr and Ole amount, by using three different techniques: direct UV spectrophotometry, High Performance Liquid Chromatography and Trolox Equivalent Antioxidant Capacity assay. The results revealed higher EE% for oleuropein. Cyto-toxicity and cyto-compatibility of liposomes were also tested on human chondrocyte cells.
没食子酸酪醇、羟基酪醇和橄榄苦苷是橄榄（Olea europaea L.）果实、叶子和油中的主要酚类化合物。这些天然抗氧化剂分子对人类健康有多种有益的影响，但生物利用度和靶向性较差。脂质体是药物/营养保健品的输送载体，用于将生物活性分子输送到目标组织，减少潜在的副作用，并保护包裹的分子免受酶代谢过程的影响。在这项研究中，合成了含有没食子酸酪醇、羟基酪醇和橄榄苦苷的两性离子脂质体，并对其粒径和表面电荷进行了表征。特别关注的是通过三种不同的技术（直接紫外分光光度法、高效液相色谱法和 Trolox 等效抗氧化能力测定法）测定包封效率（EE%），定量负载的 Tyr、HTyr 和 Ole 量。结果表明，橄榄苦苷的 EE%更高。脂质体的细胞毒性和细胞相容性也在人软骨细胞上进行了测试。
