Skin penetration enhancement by a microneedle device (Dermaroller®) in vitro: Dependency on needle size and applied formulation

Skin penetration enhancement by a microneedle device (Dermaroller®) in vitro: Dependency on needle size and applied formulation
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DOI:
10.1016/j.ejps.2008.12.008
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发表时间:
2009-03-02
影响因子:
4.6
通讯作者:
Fahr, A.
Fahr, A.
中科院分区:
医学2区
文献类型:
--
作者:
Badran, M. M.;Kuntsche, J.;Fahr, A.

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本研究主要研究一种新型微针装置(Dermaroller(R))在不同针头长度(150、500和1500微米)下对皮肤穿孔的体外评价。采用人体离体全层皮肤,研究了微针治疗对皮肤表面形态(光镜和扫描电子显微镜)、经皮失水(TEWL)和亲水性模型药物渗透和渗透的影响。此外,还比较了侵入体--含有萜烯和乙醇作为渗透促进剂的高度柔韧的磷脂微囊--与水溶液的比较。与未经处理的人皮肤相比,经Dermaroller(R)处理后的TEWL值升高,TEWL值在第一个小时内逐渐增加,而此后TEWL值下降,可能是由于孔径随时间减小所致。使用德马罗勒(R)的皮肤穿孔增强了两种被测试配方的药物渗透性和渗透性。与水溶液相比,血管小体更有效地将亲水性化合物输送到皮肤和通过皮肤,并且与皮肤穿孔相结合进一步增强了药物的渗透和渗透。总而言之,已经商业化的用于美容目的的德马罗勒(R)在药物输送方面似乎也很有前景,特别是那些针头长度中等(500微米)和更短(150微米)的药物。(C)2008爱思唯尔B.V.保留所有权利。
This study focused on the in vitro evaluation of skin perforation using a new microneedle device (Dermaroller (R)) with different needle lengths (150, 500 and 1500 mu m). The influence of the microneedle treatment on the morphology of the skin surface (studied by light and scanning electron microscopy), on the transepidermal water loss (TEWL) and on the penetration and permeation of hydrophilic model drugs was investigated using excised human full-thickness skin. Furthermore, invasomes - highly flexible phospholipid vesicles containing terpenes and ethanol as penetration enhancer - were compared with an aqueous solution. Elevated TEWL values were measured after Dermaroller (R)) treatment compared to untreated human skin with a gradual increase of the TEWL over the first hour whereas afterwards the TEWL values decreased probably caused by a reduction of the pore size with time. Skin perforation with the Dermarollers (R) enhanced drug penetration and permeation for both formulations tested. Invasomes were more effective to deliver hydrophilic compounds into and through the skin compared to the aqueous drug solutions and the combination with skin perforation further enhanced drug penetration and permeation. In conclusion, Dermarollers (R) being already commercially available for cosmetic purposes appear also promising for drug delivery purposes particularly those with medium (500 mu m) and shorter (150 mu m) needle lengths. (c) 2008 Elsevier B.V. All rights reserved.