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经皮给药系统使用无毛大鼠模型中的盘状微针辊。

Transdermal drug delivery using disk microneedle rollers in a hairless rat model.

机构信息

Department of Dermatology, Chung-Ang University College of Medicine, Seoul, South Korea.

出版信息

Int J Dermatol. 2012 Jul;51(7):859-63. doi: 10.1111/j.1365-4632.2011.05343.x.

Abstract

BACKGROUND

Transdermal drug delivery systems (TDDSs) represent more reliable and consistent methods of drug dosing than oral administration. However, TDDSs can administer only low molecular weight (MW) drugs and require a power source. Disk microneedle rollers facilitate the passage of low and high MW substances through the direct perforation of the stratum corneum and dermis, without stimulating dermal nerves.

OBJECTIVES

We investigated in vitro whether disk microneedle rollers, developed for the Diskneedle Therapy System (DTS™) in South Korea, can deliver drugs effectively through the skin of hairless rats.

METHODS

The disk microneedle rollers used in the DTS™ are metal and consist of several plates bearing microneedles of graded lengths (0.15 mm, 0.25 mm, 0.50 mm). To test in vitro permeation, the skin of a hairless rat was mounted in a Franz diffusion cell system and rolled with a disk roller without microneedles and with rollers fitted with microneedles of each size. Rhodamine B base (80 μl) was applied to the skin for 24 hours, 48 hours, and 72 hours, and dye permeation was detected at 543 nm. Dye binding to the skin was also confirmed using fluorescence microscopy at six hours after the application of rhodamine B.

RESULTS

Use of the disk microneedle roller increased the skin penetrance of rhodamine B base in hairless rats in accordance with microneedle length, as assessed using a fluorescence penetration test.

CONCLUSIONS

Disk microneedle rollers, as designed for the DTS™, can be used for transdermal drug delivery. Microneedles can be selected according to the length appropriate for each application.

摘要

背景

经皮给药系统(TDDS)比口服给药更可靠、更稳定。然而,TDDS 只能给药低分子量(MW)药物,且需要电源。盘状微针滚轮通过直接刺穿角质层和真皮来促进低和高 MW 物质的传递,而不会刺激真皮神经。

目的

我们研究了韩国开发的 Diskneedle 治疗系统(DTS)中使用的盘状微针滚轮是否可以有效地将药物递送至无毛大鼠的皮肤中。

方法

DTS 中使用的盘状微针滚轮是金属的,由多个承载不同长度微针的板组成(0.15 毫米、0.25 毫米、0.50 毫米)。为了进行体外渗透测试,将无毛大鼠的皮肤安装在 Franz 扩散细胞系统中,并用无微针和装有不同尺寸微针的滚轮进行滚压。将 80μl 的罗丹明 B 碱应用于皮肤 24 小时、48 小时和 72 小时,并在 543nm 处检测染料渗透情况。在应用罗丹明 B 六小时后,还使用荧光显微镜确认染料与皮肤的结合。

结果

使用盘状微针滚轮增加了罗丹明 B 碱在无毛大鼠皮肤中的穿透性,与微针长度成正比,这是通过荧光穿透测试评估的。

结论

为 DTS 设计的盘状微针滚轮可用于经皮药物传递。可以根据每种应用所需的长度选择微针。

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