Department of Life and Environmental Sciences, University of Cagliari, Cagliari 09124, Italy.
J Nanosci Nanotechnol. 2021 May 1;21(5):2901-2906. doi: 10.1166/jnn.2021.19047.
8-methoxypsoralen is the most common drug in psoralen plus ultraviolet light irradiation therapy for the treatment of severe psoriasis. Despite of the efficacy, its classic oral administration leads to several serious adverse effects. However, the topical psoralen application produces a drug skin accumulation lower than that obtained by oral administration, due to the drug low skin permeability. In this paper, 8-methoxypsoralen loaded Penetration Enhancer-containing Vesicles were prepared using soy phosphatidylcholine and the penetration enhancer Transcutol® (5% or 10%) and characterized in terms of size, polydispersity index, zeta potential and encapsulation efficiency. No statistically significant differences in both size (135 nm) and encapsulation efficiency (65%) were found for different Transcutol® concentration. Transdermal delivery study assessed by Franz diffusion cells, showed that the 8-methoxypsoralen mainly accumulated into the stratum corneum. Moreover, after Penetration Enhancer-containing Vesicles application, the drug recovered in this layer is almost double of that delivered by conventional liposomes, while no significant difference was found from the different Transcutol® concentrations. Finally, biocompatibility checked by an MTT assay, demonstrated that the incubation of human keratinocytes for 24 h with 8-methoxypsoralen loaded Penetration Enhancer-containing Vesicles did not significantly reduce cell viability.
8-甲氧基补骨脂素是光化学疗法中治疗严重银屑病最常用的药物。尽管有疗效，但它的经典口服给药会导致几种严重的不良反应。然而，局部应用补骨脂素会导致药物在皮肤中的蓄积低于口服给药，这是由于药物的皮肤渗透性低。本文采用大豆磷脂酰胆碱和渗透促进剂 Transcutol®（5%或 10%）制备了载 8-甲氧基补骨脂素的渗透促进剂囊泡，并对其粒径、多分散指数、Zeta 电位和包封效率进行了表征。不同 Transcutol®浓度对粒径（135nm）和包封效率（65%）均无统计学差异。Franz 扩散池的经皮传递研究表明，8-甲氧基补骨脂素主要蓄积在角质层中。此外，在应用载渗透促进剂囊泡后，该层中回收的药物几乎是普通脂质体的两倍，而不同 Transcutol®浓度之间没有明显差异。最后，通过 MTT 测定法检查的生物相容性表明，人角质形成细胞在 8-甲氧基补骨脂素载渗透促进剂囊泡中孵育 24 小时不会显著降低细胞活力。
