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采用实验设计技术制备和优化纳米转脂体,以增强缬沙坦的经皮传递。

Formulation and optimization of nanotransfersomes using experimental design technique for accentuated transdermal delivery of valsartan.

机构信息

Faculty of Pharmacy, Hamdard University, New Delhi, India.

出版信息

Nanomedicine. 2012 Feb;8(2):237-49. doi: 10.1016/j.nano.2011.06.004. Epub 2011 Jun 24.

Abstract

UNLABELLED

The purpose of this work was to develop and statistically optimize nanotransfersomes for enhanced transdermal of valsartan vis-à-vis traditional liposomes. Nanotransfersomes bearing valsartan were prepared by conventional rotary evaporation method and characterized for various parameters including entrapment efficiency, vesicles shape, size, size distribution, and skin permeation. In vivo antihypertensive activity conducted on Wistar rats was also taken as a measure of performance of nanotransfersomes and liposomes. Nanotransfersomes proved significantly superior in terms of amount of drug permeated in the skin, with an enhancement ratio of 33.97 ± 1.25 when compared to rigid liposomes. This was further confirmed through a confocal laser scanning microscopy study. Nanotransfersomes showed better antihypertensive activity in comparison to liposomes by virtue of better permeation through Wistar rat skin. Finally, it could be concluded that the nanotransfersomes accentuates the transdermal flux of valsartan and could be used as a carrier for effective transdermal delivery of valsartan.

FROM THE CLINICAL EDITOR

In this paper, the authors discuss the development and optimization of nanotransfersomes for enhanced transdermal of valsartan and demonstrate accentuated transdermal compared to standard preparations.

摘要

目的

本研究旨在开发并通过统计学方法优化纳米传递体,以增强缬沙坦的经皮渗透,优于传统脂质体。通过常规旋转蒸发法制备载有缬沙坦的纳米传递体,并对各种参数进行表征,包括包封率、囊泡形态、粒径、粒径分布和皮肤渗透。还将 Wistar 大鼠的体内降压活性作为纳米传递体和脂质体性能的衡量标准。与刚性脂质体相比,纳米传递体在皮肤中渗透的药物量显著增加,增强比为 33.97±1.25。这通过共聚焦激光扫描显微镜研究进一步得到证实。纳米传递体通过更好地穿透 Wistar 大鼠皮肤,表现出比脂质体更好的降压活性。最后,可以得出结论,纳米传递体可以增强缬沙坦的经皮渗透,可作为缬沙坦有效经皮给药的载体。

临床编辑按

在本文中,作者讨论了开发和优化纳米传递体以增强缬沙坦的经皮渗透,并证明与标准制剂相比,经皮渗透能力增强。

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