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无针注射器向皮肤递药的可能性和效果。

Possibility and effectiveness of drug delivery to skin by needle-free injector.

机构信息

Department of Pharmacy Services, Saitama Medical School, Medical Center, 1981 Kamoda, Kawagoe, Saitama 350-8550, Japan.

出版信息

Int J Pharm. 2010 May 31;391(1-2):65-72. doi: 10.1016/j.ijpharm.2010.02.019. Epub 2010 Feb 17.

DOI:10.1016/j.ijpharm.2010.02.019
PMID:20170719
Abstract

We evaluated a needle-free injector (NFI), which has been studied as an administration device to the subcutaneous tissue, as a device to deliver drugs into skin tissues. ShimaJet used for self-injection of insulin was selected as a spring-powered NFI in this study. Weak (NFI-w) and strong (NFI-s) injectors were evaluated. Rhodamine 6G, as a model compound, was injected onto the skin surface of hairless rats and the skin distribution and amount released from the skin of the compound were followed. A modified nozzle (able to inject at an angle of 45 degrees ) was prepared in addition to the conventional dedicated nozzle. The spring constants, nozzle shapes and penetration enhancer, 1-[2-(decylthio)ethyl] azacyclopentane-2-one (HPE-101), affected not only the skin distribution, but also the release profiles of rhodamine 6G. In addition, the release profiles of rhodamine 6G after injection using NFI-w or NFI-s obeyed diffusion-controlled or membrane-controlled kinetics, respectively. This difference was probably due to the skin site (depth) of rhodamine 6G delivered by the NFI. Furthermore, HPE-101 increased the retention time of rhodamine 6G in the epidermis. The present results suggested that an NFI can be a useful tool for enhanced drug delivery into skin.

摘要

我们评估了一种无针注射器 (NFI),它已被研究作为一种向皮下组织给药的装置,也可作为一种将药物递送至皮肤组织的装置。在本研究中,选择了 ShimaJet 作为用于自行注射胰岛素的弹簧驱动 NFI。评估了弱 (NFI-w) 和强 (NFI-s) 注射器。将罗丹明 6G 作为模型化合物注射到无毛大鼠的皮肤表面上,并跟踪该化合物在皮肤中的分布和释放量。除了常规专用喷嘴外,还制备了一种改良的喷嘴(能够以 45 度角注射)。弹簧常数、喷嘴形状和渗透增强剂 1-[2-(癸硫基)乙基]氮杂环戊烷-2-酮 (HPE-101) 不仅影响皮肤分布,还影响罗丹明 6G 的释放曲线。此外,使用 NFI-w 或 NFI-s 注射后罗丹明 6G 的释放曲线分别遵循扩散控制或膜控制动力学。这种差异可能是由于 NFI 输送的罗丹明 6G 的皮肤部位(深度)不同。此外,HPE-101 增加了罗丹明 6G 在表皮中的滞留时间。本研究结果表明,NFI 可以成为增强药物递送至皮肤的有用工具。

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