• 主题
高级搜索  >
历史搜索 清空历史
首页> 美国卫生研究院文献>Drug Delivery >Permeation-enhancing effects and mechanisms of O-acylterpineol on isosorbide dinitrate: mechanistic insights based on ATR-FTIR spectroscopy molecular modeling and CLSM images
【2h】

Permeation-enhancing effects and mechanisms of O-acylterpineol on isosorbide dinitrate: mechanistic insights based on ATR-FTIR spectroscopy molecular modeling and CLSM images

机译：O-酰基松油醇对硝酸异山梨酯的渗透增强作用和机理：基于ATR-FTIR光谱分子建模和CLSM图像的机理见解

代理获取
本网站仅为用户提供外文OA文献查询和代理获取服务，本网站没有原文。下单后我们将采用程序或人工为您竭诚获取高质量的原文，但由于OA文献来源多样且变更频繁，仍可能出现获取不到、文献不完整或与标题不符等情况，如果获取不到我们将提供退款服务。请知悉。
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

The present study aimed to evaluate the penetration activity of O-acylterpineol derivatives both in vitro and in vivo, and to investigate the enhancing mechanism of O-acylterpineol derivatives which were synthesized by α-terpineol and fatty acid. The promoting activities on the isosorbide dinitrate patch were tested across full thickness rabbit skin both in vitro and in vivo. In order to elucidate the permeation mechanism, attenuated total reflection Fourier transform infrared spectroscopy, molecular modeling, and confocal laser scanning microscopy were introduced to investigate the regulation of enhancers in the skin permeability and biophysical properties. With in vitro cytotoxicity test and in vivo erythema model, the skin irritation of enhancers was also evaluated. Permeation studies showed 2-(4-methylcyclohex-3-en-l-yl) propan-2-yl tetradecanoate produced the obvious enhancement activity for ISDN both in vitro and in vivo from patches. These results were supported by ATR-FTIR, molecular modeling, and CLSM studies which revealed that O-acylterpineol could decrease the order of the alkyl chains in the skin lipids. Additionally, it was found that TER-C14 produced a relatively low skin irritation, compared with the TER which was assumed to be a safe compound. The present research suggested that some newly designed acylterpineol derivatives are shown to be suitable permeation enhancers for transdermal drug delivery, and the chain length of C14 seem to be safe and more favorable for the penetration of ISDN from DIA patches.
机译：本研究旨在评估O-酰基松油醇衍生物在体内外的渗透活性，并研究α-萜品醇和脂肪酸合成的O-酰基松油醇衍生物的增强机理。在体外和体内在全厚度的兔皮肤上测试了对硝酸异山梨酯贴剂的促进活性。为了阐明渗透机制，引入了衰减全反射傅立叶变换红外光谱，分子建模和共聚焦激光扫描显微镜，以研究增强剂在皮肤渗透性和生物物理特性方面的调节。通过体外细胞毒性测试和体内红斑模型，还评估了增强剂对皮肤的刺激性。渗透研究表明2-（4-甲基环己基-3-烯-1-基）丙-2-基十四烷酸酯在斑块内和体外均对ISDN产生明显的增强活性。这些结果得到ATR-FTIR，分子模型和CLSM研究的支持，这些研究表明O-酰基松油醇可以降低皮肤脂质中烷基链的顺序。另外，发现TER-C14与被认为是安全化合物的TER相比产生了相对较低的皮肤刺激。本研究表明，一些新设计的酰基松油醇衍生物是适合透皮给药的渗透增强剂，C14的链长似乎是安全的，并且更有利于ISDN从DIA贴片中渗透。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
代理获取

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号