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评估微针阵列在经皮给药皮肤预处理中的针长和密度。

Evaluation needle length and density of microneedle arrays in the pretreatment of skin for transdermal drug delivery.

机构信息

Department of Biomedical and Pharmaceutical Sciences, Idaho State University, 970 S 5th Ave, Stop 8334, Pocatello, ID 83209, United States.

出版信息

Int J Pharm. 2010 May 31;391(1-2):7-12. doi: 10.1016/j.ijpharm.2010.02.007. Epub 2010 Feb 25.

DOI:10.1016/j.ijpharm.2010.02.007
PMID:20188808
Abstract

Solid silicon microneedle arrays with different needle lengths (ranging from 100 to 1100 microm) and needle densities (ranging from 400 to 11,900 needles/cm(2)) were used to penetrate epidermal membrane of human cadaver skin. After this pretreatment, the electrical resistance of the skin and the flux of acyclovir across the skin were monitored. A linear correlation between the acyclovir flux and the inverse of the skin electric resistance was observed. Microneedle arrays with longer needles (>600 microm) were more effective in creating pathways across skin and enhancing drug flux, and microneedle arrays with lower needle densities (<2000 needles/cm(2)) were more effective in enhancing drug flux if the microneedles with long enough needle length (>600 microm). In addition, the microneedle arrays were used to penetrate hairless rat skin in vivo, and the trans-epidermal water loss (TEWL) of the rat skin was measured before and after the pretreatment. Treating rat skin with microneedle arrays of lower needle density and longer needle length was more effective in increasing TEWL. Integrity of the stratum corneum barrier of the penetrated rat skin as measured by TEWL recovered back to its base line level within 24h after the microneedle pretreatment.

摘要

采用不同长度(100 至 1100 微米)和密度(400 至 11900 根/平方厘米)的固态硅微针阵列穿刺人体尸体皮肤的表皮膜。预处理后,监测皮肤的电阻和阿昔洛韦的电渗流量。阿昔洛韦的通量与皮肤电阻的倒数呈线性相关。较长的(>600 微米)微针阵列在创建跨皮肤的通路和增强药物通量方面更有效,而较低的(<2000 根/平方厘米)微针密度在微针足够长(>600 微米)的情况下更有效增强药物通量。此外,微针阵列还用于活体无毛大鼠皮肤的穿刺,在预处理前后测量大鼠皮肤的经皮水分流失(TEWL)。用低针密度和长针长度的微针阵列处理大鼠皮肤,更有效地增加 TEWL。经微针预处理 24 小时后,通过 TEWL 测量,穿透的大鼠皮肤角质层屏障的完整性恢复到基线水平。

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