Department of Neurosciences, Biomedicine and Movement Sciences, University of Verona, I-37134 Verona, Italy.
Department of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, I-44121 Ferrara, Italy.
Int J Mol Sci. 2021 May 19;22(10):5341. doi: 10.3390/ijms22105341.
In this pilot study, ethosomes and transethosomes were investigated as potential delivery systems for cholecalciferol (vitamin D3), whose deficiency has been correlated to many disorders such as dermatological diseases, systemic infections, cancer and sarcopenia. A formulative study on the influence of pharmaceutically acceptable ionic and non-ionic surfactants allowed the preparation of different transethosomes. In vitro cytotoxicity was evaluated in different cell types representative of epithelial, connective and muscle tissue. Then, the selected nanocarriers were further investigated at light and transmission electron microscopy to evaluate their uptake and intracellular fate. Both ethosomes and transethosomes proven to have physicochemical properties optimal for transdermal penetration and efficient vitamin D3 loading; moreover, nanocarriers were easily internalized by all cell types, although they followed distinct intracellular fates: ethosomes persisted for long times inside the cytoplasm, without inducing subcellular alteration, while transethosomes underwent rapid degradation giving rise to an intracellular accumulation of lipids. These basic results provide a solid scientific background to in vivo investigations aimed at exploring the efficacy of vitamin D3 transdermal administration in different experimental and pathological conditions.
在这项初步研究中，我们研究了醇质体和转醇质体作为胆钙化醇（维生素 D3）的潜在传递系统，维生素 D3 的缺乏与许多疾病有关，如皮肤病、全身感染、癌症和肌肉减少症。通过对药用可接受的离子型和非离子型表面活性剂的制剂研究，我们制备了不同的转醇质体。在体外，我们在不同的细胞类型中评估了细胞毒性，这些细胞类型代表了上皮、结缔和肌肉组织。然后，我们进一步用光镜和透射电子显微镜研究了选定的纳米载体，以评估它们的摄取和细胞内命运。醇质体和转醇质体都被证明具有最佳的物理化学性质，可促进透皮渗透和高效负载维生素 D3；此外，纳米载体很容易被所有细胞类型内化，尽管它们遵循不同的细胞内命运：醇质体在细胞质中长时间存在，不会引起亚细胞改变，而转醇质体则迅速降解，导致细胞内脂质积累。这些基础结果为探索不同实验和病理条件下维生素 D3 经皮给药疗效的体内研究提供了坚实的科学基础。
