In Vitro Skin Absorption of the Topically Applied Metal Ion-Chelating Agent Diethylenetriaminepenta-acetic Acid

R. Pendlington, E. J. Brown, D. Sanders, H. Minter, S. Hyde, M. Snow, C. K. Smith Pease
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Abstract

Diethylenetriaminepenta-acetic acid (DTPA) is a metal ion-chelating agent that has antimicrobial properties and potential therapeutic properties against metal-induced toxicities such as nickel allergy. In this study, the absorption properties of DTPA applied topically to rat skin are investigated in vitro, using a flow-through diffusion skin absorption model. [14C]DTPA was applied in solution in 60% ethanol (pH 6). Overall skin penetration into receptor fluid resulting from a topical dose of 0.13 mg/cm2 DTPA for 24 h was low at 1.27%. The local tissue distribution of DTPA was investigated using microautoradiography, and effects on the tissue were assessed by histology. Diethylenetriaminepenta-acetic acid was primarily associated with the stratum corneum and upper layers of the skin; minimal levels were observed in the dermis.
外用金属离子螯合剂二乙烯三胺五乙酸的体外皮肤吸收
二乙烯三胺五乙酸(DTPA)是一种金属离子螯合剂,具有抗菌性能和治疗镍过敏等金属毒性的潜在性能。本研究采用体外流动扩散皮肤吸收模型,对大鼠皮肤外用DTPA的吸收特性进行了研究。[14C]将DTPA应用于60%乙醇(pH 6)的溶液中。局部剂量为0.13 mg/cm2的DTPA持续24小时后,皮肤对受体液的整体渗透较低,为1.27%。应用显微放射自显影术研究DTPA的局部组织分布,并用组织学方法评估其对组织的影响。二乙烯三胺五乙酸主要与角质层和皮肤上层有关;在真皮中观察到最低水平。
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