The effect of microneedles on the skin permeability and antitumor activity of topical 5-fluorouracil.
The effect of microneedles on the skin permeability and antitumor activity of topical 5-fluorouracil.
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DOI：
10.1016/j.apsb.2013.12.013
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发表时间：
2014-02-01
影响因子：
14.5
通讯作者：
Cuin, Zhengrong
中科院分区：
文献类型：
--
作者：
Naguib, Youssef W.;Kumar, Amit;Cuin, Zhengrong
关键词：
局部5-氟尿嘧啶（5-FU）被批准用于治疗浅表基底细胞癌和光化性角化病。然而，5-FU的皮肤渗透性较差。微针已成功应用于通过在皮肤角质层中形成微米大小的孔来改善小分子和大分子甚至纳米颗粒的皮肤渗透性。在本报告中，测试了使用微针增加5-FU皮肤渗透性的可行性。使用安装在 Franz 扩散装置上的全厚小鼠皮肤，结果表明，当用微针（长度为 500 μm，基底直径为 50 μm）预处理皮肤时，5-FU 通过皮肤的通量增加了 4.5 倍。在皮下植入 B16-F10 小鼠黑色素瘤细胞的小鼠模型中，与仅将乳膏涂抹在植入了肿瘤细胞的皮肤区域且未经微针预处理的皮肤区域相比，将市售 5-FU 外用乳膏（5%）涂抹在经过微针预处理的皮肤区域时，其抗肿瘤活性显着增强。氟尿嘧啶尚未被批准用于黑色素瘤治疗，但通过将微针技术融入治疗中，可以提高局部 5-FU 针对基底细胞癌等肿瘤的临床疗效。用微针预处理小鼠皮肤可显着增加体外 5-氟尿嘧啶 (5-FU) 的皮肤渗透性（左），并增强局部应用 5-FU 对皮下植入小鼠体内的 B16-F10 小鼠黑色素瘤细胞的抗肿瘤活性（右）。
Topical 5-fluorouracil (5-FU) is approved for the treatment of superficial basal cell carcinoma and actinic keratosis. However, 5-FU suffers from poor skin permeation. Microneedles have been successfully applied to improve the skin permeability of small and large molecules, and even nanoparticles, by creating micron-sized pores in the stratum corneum layer of the skin. In this report, the feasibility of using microneedles to increase the skin permeability of 5-FU was tested. Using full thickness mouse skin mounted on Franz diffusion apparatus, it was shown that the flux of 5-FU through the skin was increased by up to 4.5-fold when the skin was pretreated with microneedles (500 μm in length, 50 μm in base diameter). In a mouse model with B16-F10 mouse melanoma cells implanted in the subcutaneous space, the antitumor activity of a commercially available 5-FU topical cream (5%) was significantly enhanced when the cream was applied on a skin area that was pretreated with microneedles, as compared to when the cream was simply applied on a skin area, underneath which the tumor cells were implanted, and without pretreatment of the skin with microneedles. Fluorouracil is not approved for melanoma therapy, but the clinical efficacy of topical 5-FU against tumors such as basal cell carcinoma may be improved by integrating microneedle technology into the therapy. Pretreatment of mouse skin with microneedles significantly increased the skin permeability of 5-fluorouracil (5-FU) in vitro (left), and enhanced the antitumor activity of topically applied 5-FU against B16-F10 mouse melanoma cells implanted subcutaneously in mice (right).
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影响因子：
8
作者：
Kumar A;Li X;Sandoval MA;Rodriguez BL;Sloat BR;Cui Z
通讯作者：
Cui Z
影响因子：
1.4
作者：
DEKEIZER, RJW;DEWOLFFROUENDAAL, D;VANDELFT, JL
通讯作者：
VANDELFT, JL
影响因子：
11.2
作者：
Sabitha, M.;Rejinold, N. Sanoj;Jayakumar, R.
通讯作者：
Jayakumar, R.
影响因子：
5.8
作者：
Fang, JY;Hung, CF;Chan, TF
通讯作者：
Chan, TF
影响因子：
1.7
作者：
Takahashi, H;Funabiki, K;Takasaki, K
通讯作者：
Takasaki, K