PDF(Pubmed)
Abstract：
The efficacy of nanostructured lipid carriers (NLC) for drug delivery strongly depends on their stability and cell uptake. Both properties are governed by their compositions and internal structure. To test the effect of the lipid composition of NLC on cell uptake and stability, three kinds of liquid lipids with different degrees of unsaturation are employed. After ensuring homogeneous size distributions, the thermodynamic characteristics, stability, and mixing properties of NLC are characterized. Then the rates and predominant pathways of cell uptake are determined. Although the same surfactant is used in all cases, different uptake rates are observed. This finding contradicts the view that the surface properties of NLC are dominated by the surfactant. Instead, the uptake rates are explained by the structure of the nanocarrier. Depending on the mixing properties, some liquid lipids remain inside the nanocarrier, while other liquid lipids are present on the surface. Nanocarriers with liquid lipids on the surface are taken up more readily by the cells. This shows that the engineering of efficient lipid nanocarriers requires a delicate balance of interactions between all components of the nanocarrier on the molecular level.
摘要：
纳米结构脂质载体(NLC)用于药物递送的功效强烈依赖于它们的稳定性和细胞摄取。这两种性质都由它们的组成和内部结构决定。为了测试NLC的脂质组成对细胞摄取和稳定性的影响，使用三种不饱和度不同的液体脂质。在确保均匀的尺寸分布后，热力学特性，稳定性,并对NLC的混合性能进行了表征。然后确定细胞摄取的速率和主要途径。尽管在所有情况下都使用相同的表面活性剂，观察到不同的摄取率。该发现与NLC的表面性质受表面活性剂支配的观点相矛盾。相反，吸收速率由纳米载体的结构解释。根据混合特性，一些液体脂质留在纳米载体内，而其他液体脂质存在于表面。表面上具有液体脂质的纳米载体更容易被细胞吸收。这表明,高效脂质纳米载体的工程化需要纳米载体的所有组分之间在分子水平上的相互作用的微妙平衡。
