Center for Drug Delivery Research, Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA 30341, USA.
CFD Research Corporation, 701 McMillian Way, Huntsville, AL 35806, USA.
Int J Pharm. 2022 Apr 25;618:121693. doi: 10.1016/j.ijpharm.2022.121693. Epub 2022 Mar 21.
Psoriasis is a condition of the skin which involves scales, dry patches, and inflammation. Methotrexate (logP: -1.8, MW:454.44 g/mol) is administered orally or intravenously to treat psoriasis. The first-pass metabolism and systemic toxicity can be avoided by administration via skin. Topical and transdermal delivery of methotrexate using iontophoresis and microneedles, alone and in combination was investigated using full-thickness healthy human skin. It is also equally relevant to evaluate the delivery into and across damaged/diseased skin. Hence, this study investigated the delivery of methotrexate using ex vivo healthy and psoriatic human skin to understand the effect of skin disease condition on delivery of methotrexate via skin. A lower resistance and a higher TEWL for psoriatic skin indicated damaged barrier function, while histology studies indicated epithelial hyperproliferation and elongated rete ridges. Using the optimized iontophoretic parameters, there was no significant difference in receptor delivery for psoriatic skin (39.51 ± 4.45 µg/sq.cm) as compared to healthy skin (43.15 ± 0.83 µg/sq.cm). However, methotrexate delivery into psoriatic skin (126.23 ± 24.65 µg/sq.cm) was significantly higher as compared to healthy skin (12.02 ± 4.89 µg/sq.cm). Thus, significantly higher total delivery was observed from psoriatic skin than healthy skin.
银屑病是一种皮肤疾病,其特征为鳞屑、干燥斑块和炎症。甲氨蝶呤(logP:-1.8,MW:454.44 g/mol)通过口服或静脉注射用于治疗银屑病。通过皮肤给药可以避免首过代谢和全身毒性。本文通过离子电渗和微针单独和联合使用,研究了甲氨蝶呤的透皮和经皮给药,研究对象为全厚健康人体皮肤。评估进入和穿过受损/患病皮肤的药物输送同样具有重要意义。因此,本研究使用离体健康和银屑病人类皮肤来研究甲氨蝶呤的输送,以了解皮肤疾病状况对皮肤输送甲氨蝶呤的影响。银屑病皮肤的电阻较低,TEWL 较高,表明其屏障功能受损,而组织学研究表明上皮细胞过度增生和延长的 rete ridges。使用优化的离子电渗参数,与健康皮肤(43.15±0.83μg/sq.cm)相比,银屑病皮肤的受体输送(39.51±4.45μg/sq.cm)没有显著差异。然而,与健康皮肤(12.02±4.89μg/sq.cm)相比,甲氨蝶呤输送到银屑病皮肤(126.23±24.65μg/sq.cm)的量显著增加。因此,从银屑病皮肤观察到的总药物输送量显著高于健康皮肤。