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Effect of Iontophoresis on the Intradermal Migration Rate of Medium Molecular Weight Drugs
Chemical & Pharmaceutical Bulletin ( IF 1.5 ) Pub Date : 2021-07-01 , DOI: 10.1248/cpb.c21-00131
Kenji Sugibayashi 1, 2 , Mika Futaki 1 , Miyu Hashimoto 1 , Asuka Fukuhara 1 , Kengo Matsumoto 1 , Takeshi Oshizaka 2 , Shoko Itakura 1 , Hiroaki Todo 1
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The purpose of the present study was to evaluate whether iontophoresis (IP) accelerates the intradermal migration rate of medium molecular weight drugs. Sodium polystyrene sulfonate (PSA) and fluorescein isothiocyanate-dextran (FD) were used as model medium molecular weight acidic and non-electrolyte drugs, respectively. Low molecular weight acid and non-electrolyte drugs were also used for comparison. Drug-loaded excised split-layered skin (SL skin) was used in the experiment. SL skin was prepared using (i) whole skin was split once, (ii) the drug solution was applied on the lower skin, and (iii) the upper skin was layered onto the lower skin containing the drug solution as in the original skin. The effect of constant-current cathodal or anodal IP was applied to the SL skin, and the time course of the cumulative amount of drug migration from the SL skin through the dermis to the receiver was followed. In cases without IP and with anodal IP, the intradermal migration rates of medium molecular weight drugs were much lower than those of small molecules. The driving force for drug migration was thought to be simple diffusion through the skin layer. In contrast, cathodal IP significantly increased the intradermal migration rate of PSA not but of FD or low molecular weight drugs. This IP-facilitated migration of PSA was probably due to electrorepulsion. These results suggest that IP can be used to increase the intradermal migration of medium molecular weight charged drugs.

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中文翻译:

离子电渗疗法对中等分子量药物皮内迁移率的影响

本研究的目的是评估离子电渗疗法 (IP) 是否会加速中等分子量药物的皮内迁移速度。聚苯乙烯磺酸钠 (PSA) 和异硫氰酸荧光素-葡聚糖 (FD) 分别用作模型中等分子量酸性和非电解质药物。低分子量酸和非电解质药物也用于比较。实验中使用载药切除的分层皮肤(SL皮肤)。SL皮肤是这样制备的:(i)将整个皮肤分开一次,(ii)将药物溶液涂在下层皮肤上,(iii)上层皮肤与原始皮肤一样,在含有药物溶液的下层皮肤上分层。恒流阴极或阳极IP的效果应用于SL皮肤,跟踪药物从 SL 皮肤通过真皮到接受者的累积量的时间过程。在没有 IP 和阳极 IP 的情况下,中等分子量药物的皮内迁移率远低于小分子。药物迁移的驱动力被认为是通过皮肤层的简单扩散。相比之下,阴极 IP 显着增加了 PSA 的皮内迁移率,而不是 FD 或低分子量药物。这种 IP 促进的 PSA 迁移可能是由于电排斥。这些结果表明 IP 可用于增加中等分子量带电药物的皮内迁移。中分子药物的皮内迁移率远低于小分子药物。药物迁移的驱动力被认为是通过皮肤层的简单扩散。相比之下,阴极 IP 显着增加了 PSA 的皮内迁移率,而不是 FD 或低分子量药物。这种 IP 促进的 PSA 迁移可能是由于电排斥。这些结果表明 IP 可用于增加中等分子量带电药物的皮内迁移。中分子药物的皮内迁移率远低于小分子药物。药物迁移的驱动力被认为是通过皮肤层的简单扩散。相比之下,阴极 IP 显着增加了 PSA 的皮内迁移率,而不是 FD 或低分子量药物。这种 IP 促进的 PSA 迁移可能是由于电排斥。这些结果表明 IP 可用于增加中等分子量带电药物的皮内迁移。这种 IP 促进的 PSA 迁移可能是由于电排斥。这些结果表明 IP 可用于增加中等分子量带电药物的皮内迁移。这种 IP 促进的 PSA 迁移可能是由于电排斥。这些结果表明 IP 可用于增加中等分子量带电药物的皮内迁移。

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更新日期:2021-06-30
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