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微针对选定抗高血压药物(盐酸地尔硫䓬和培哚普利叔丁胺盐)经皮渗透的影响。

The Influence of Microneedles on the Percutaneous Penetration of Selected Antihypertensive Agents: Diltiazem Hydrochloride and Perindopril Erbumine.

作者信息

Luu Emmy, Ita Kevin B, Morra Matthew J, Popova Inna E

机构信息

College of Pharmacy, Touro University California, Mare Island-Vallejo, CA, United States.

Department of Soil and Water Systems, University of Idaho, Moscow, Idaho, ID 83844-2339, United States.

出版信息

Curr Drug Deliv. 2018;15(10):1449-1458. doi: 10.2174/1567201815666180730125941.

Abstract

BACKGROUND

It is well documented in the scientific literature that high blood pressure can lead to cardiovascular disease. Untreated hypertension has clinical consequences such as coronary artery disease, stroke or kidney failure. Diltiazem hydrochloride (DH), a calcium-channel blocker, and perindopril erbumine (PE), an inhibitor of the angiotensin converting enzyme are used for the management of hypertension.

OBJECTIVE

This project will examine the effect of microneedle rollers on the transport of DH and PE across pig ear skin. The use of the transcutaneous route of administration reduces and in sometimes eliminates the trauma and pain associated with injections. Furthermore, there is increased patient compliance. The purpose of this project was to study the effect of stainless steel microneedles on the transdermal delivery of DH and PE.

METHOD

We utilized vertical Franz diffusion cells to study in vitro transport of DH and PE across microneedle- treated pig ear skin. Confocal laser scanning microscopy (CLSM) was used to characterize microchannel depth. Transdermal flux values were determined from the slope of the linear portion of the cumulative amount versus time curve.

RESULTS

There was a 113.59-fold increase in the transdermal permeation of DH following the application of microneedle roller compared to passive diffusion.

CONCLUSION

In the case of PE, there was an 11.99-fold increase in the drug transport across pig skin following the application of microneedle rollers in comparison with passive diffusion. Student's t-test and Mann-Whitney's rank sum test were used to determine statistically significant differences between experimental and control groups.

摘要

背景

科学文献充分证明,高血压可导致心血管疾病。未经治疗的高血压会产生诸如冠状动脉疾病、中风或肾衰竭等临床后果。盐酸地尔硫䓬(DH)是一种钙通道阻滞剂,培哚普利叔丁胺盐(PE)是一种血管紧张素转换酶抑制剂,二者均用于高血压的治疗。

目的

本项目将研究微针滚轮对DH和PE透过猪耳皮肤转运的影响。采用经皮给药途径可减少甚至有时消除与注射相关的创伤和疼痛。此外,患者的依从性也会提高。本项目的目的是研究不锈钢微针对DH和PE经皮给药的影响。

方法

我们利用垂直式Franz扩散池研究DH和PE在经微针处理的猪耳皮肤上的体外转运。采用共聚焦激光扫描显微镜(CLSM)表征微通道深度。经皮通量值由累积量与时间曲线线性部分的斜率确定。

结果

与被动扩散相比,应用微针滚轮后DH的经皮渗透增加了113.59倍。

结论

对于PE,与被动扩散相比,应用微针滚轮后药物在猪皮肤上的转运增加了11.99倍。采用学生t检验和曼-惠特尼秩和检验来确定实验组与对照组之间的统计学显著差异。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd78/6340158/7a8584faaab0/CDD-15-1449_F1.jpg

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