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Idebenone-loaded solid lipid nanoparticles for drug delivery to the skin: In vitro evaluation

机译:载有艾地苯醌的固体脂质纳米颗粒,用于向皮肤输送药物:体外评估

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摘要

Idebenone (IDE), a synthetic derivative of ubiquinone, shows a potent antioxidant activity that could be beneficial in the treatment of skin oxidative damages. In this work, the feasibility of targeting IDE into the upper layers of the skin by topical application of IDE-loaded solid lipid nanoparticles (SLN) was evaluated. SLN loading different amounts of IDE were prepared by the phase inversion temperature method using cetyl palmitate as solid lipid and three different non-ionic surfactants: ceteth-20, isoceteth-20 and oleth-20. All IDE loaded SLN showed a mean particle size in the range of 30-49 nm and a single peak in size distribution. In vitro permeation/penetration experiments were performed on pig skin using Franz-type diffusion cells. IDE penetration into the different skin layers depended on the type of SLN used while no IDE permeation occurred from all the SLN under investigation. The highest IDE content was found in the epidermis when SLN contained ceteth-20 or isoceteth-20 as surfactant while IDE distribution into the upper skin layers depended on the amount of IDE loaded when oleth-20 was used as surfactant. These results suggest that the SLN tested could be an interesting carrier for IDE targeting to the upper skin layers.
机译:艾地苯醌(IDE)是泛醌的合成衍生物,具有强大的抗氧化活性,可能有益于治疗皮肤氧化损伤。在这项工作中,评估了通过局部应用载有IDE的固体脂质纳米颗粒(SLN)将IDE靶向皮肤上层的可行性。通过相转变温度法使用棕榈酸十六烷基酯作为固体脂质和三种不同的非离子表面活性剂:ceteth-20,isoceteth-20和oleth-20,制备了负载不同量IDE的SLN。所有IDE加载的SLN的平均粒径均在30-49 nm范围内,并且粒径分布只有一个峰。使用Franz型扩散池在猪皮肤上进行了体外渗透/渗透实验。 IDE能否渗透到不同的皮肤层中取决于所使用的SLN的类型,而所研究的所有SLN都不会发生IDE渗透。当SLN含有ceteth-20或isoceteth-20作为表面活性剂时,表皮中的IDE含量最高,而IDE分配到上皮层的程度取决于使用oleth-20作为表面活性剂时IDE的负载量。这些结果表明,所测试的SLN可能是将IDE定位到上层皮肤层的有趣载体。

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