Transdermal Delivery of Iron Using Soluble Microneedles: Dermal Kinetics and Safety.
Transdermal Delivery of Iron Using Soluble Microneedles: Dermal Kinetics and Safety.
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DOI：
10.1016/j.xphs.2015.12.008
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发表时间：
2016-03
影响因子：
3.8
通讯作者：
Murthy SN
中科院分区：
文献类型：
--
作者：
Modepalli N;Shivakumar HN;McCrudden MT;Donnelly RF;Banga A;Murthy SN
目前，所有年龄段的患者都通过口服和非肠道途径服用铁化合物，以治疗铁缺乏。尽管通过这些传统途径继续努力补充铁，但缺铁仍然是世界上最普遍的营养障碍。经皮补铁是一种新的、有潜力的补铁途径。焦磷酸铁(FPP)被发现是一种适合于经皮补充的铁源。本项目通过用高浓度的FPP刺激真皮成纤维细胞来评估FPP的安全性。进行细胞存活率测定和活性氧测定。研制了含有FPP的可溶性微针阵列，研究了微针阵列在无毛大鼠皮肤中的游离铁动力学；研究了微针阵列经皮给药后的细胞外液。从基于细胞的分析中，FPP被选为潜在的经皮给药铁源之一。这些微针被发现在给药后3小时内溶解在皮肤液中。微针阵列完全溶解后，真皮细胞外液中FPP浓度下降。总体而言，这些研究证明了FPP经皮给药的安全性，以及可溶微针途径用于经皮铁补充治疗的可行性。
Currently, the iron compounds are administered via oral and parenteral routes in patients of all ages, to treat iron deficiency. Despite continued efforts to supplement iron via these conventional routes, iron deficiency still remains the most prevalent nutritional disorder all over the world. Transdermal replenishment of iron is a novel, potential approach of iron replenishment. Ferric pyrophosphate (FPP) was found to be a suitable source of iron for transdermal replenishment. The safety of FPP was assessed in this project by challenging the dermal fibroblast cells with high concentration of FPP. The cell viability assay and reactive oxygen species assay were performed. The soluble microneedle array was developed, incorporated with FPP and the kinetics of free iron in the skin; extracellular fluid following dermal administration of microneedle array was investigated in hairless rats. From the cell based assays, FPP was selected as one of the potential iron sources for transdermal delivery. The microneedles were found to dissolve in the skin fluid within 3 hours of administration. The FPP concentration in the dermal extracellular fluid declined after complete dissolution of the microneedle array. Overall, the studies demonstrated the safety of FPP for dermal delivery and the feasibility of soluble microneedle approach for transdermal iron replenishment therapy.