用于布洛芬透皮给药的 Emulgel 和纳米结构脂质载体凝胶配方的评估:表征、机械性能和体内外皮肤渗透。

IF 4.3 3区 材料科学 Q1 ENGINEERING, ELECTRICAL & ELECTRONIC
Duygu Yılmaz Usta, Zeynep Safak Teksin, Fatmanur Tugcu-Demiroz
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引用次数: 0

摘要

在非甾体抗炎药的透皮应用中,剂型的流变学和机械特性会影响药物的性能。本研究旨在开发含布洛芬的凝胶配方和基于纳米结构脂质载体 NLC 的凝胶配方,评估其机械性能、生物黏附性和体内外兔子皮肤渗透性。所有制剂都表现出非牛顿假塑性行为,其粘度值适合局部应用。纳米结构脂质载体系统的粒径为 468 ± 21 nm,封装效率为 95.58 ± 0.41%。根据背挤压研究得出的粘度指数、稠度、坚固度和内聚力值,发现 E2 配方更适合透皮应用。粘度值最高的 E2 配方的坚固性和剪切力值也最高,因此被选为最适合进行铺展性测试的配方。NLC 基凝胶和 IBU 负载 NLC 基凝胶的生物黏附功值分别为 0.226 ± 0.028 和 0.181 ± 0.006 mJ/cm2。24 小时后,Ibuactive-Cream 和 E2 中的 IBU 穿透兔皮肤的百分比分别为 87.4 ± 2.11% 和 93.4 ± 2.72%。在对布洛芬的皮肤渗透性进行评估时,发现 E2 制剂因其脂质和纳米颗粒结构而增加了渗透性。综上所述,以 NLC 为基础的凝胶制剂可提高疗效,是一种很好的透皮制剂替代品。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Evaluation of Emulgel and Nanostructured Lipid Carrier-Based Gel Formulations for Transdermal Administration of Ibuprofen: Characterization, Mechanical Properties, and Ex-Vivo Skin Permeation

Evaluation of Emulgel and Nanostructured Lipid Carrier-Based Gel Formulations for Transdermal Administration of Ibuprofen: Characterization, Mechanical Properties, and Ex-Vivo Skin Permeation

In transdermal applications of nonsteroidal anti-inflammatory drugs, the rheological and mechanical properties of the dosage form affect the performance of the drug. The aim of this study to develop emulgel and nanostructured lipid carrier NLC-based gel formulations containing ibuprofen, evaluate their mechanical properties, bioadhesive value and ex-vivo rabbit skin permeability. All formulations showed non-Newtonian pseudoplastic behavior and their viscosity values are suitable for topical application. The particle size of the nanostructured lipid carrier system was found to be 468 ± 21 nm, and the encapsulation efficiency was 95.58 ± 0.41%. According to the index of viscosity, consistency, firmness, and cohesiveness values obtained as a result of the back extrusion study, E2 formulation was found to be more suitable for transdermal application. The firmness and work of shear values of the E2 formulation, which has the highest viscosity value, were also found to be the highest and it was chosen as the most suitable formulation in terms of the spreadability test. The work of bioadhesion values of NLC-based gel and IBU-loaded NLC-based gel were found as 0.226 ± 0.028 and 0.181 ± 0.006 mJ/cm2 respectively. The percentages of IBU that penetrated through rabbit skin from the Ibuactive-Cream and the E2 were 87.4 ± 2.11% and 93.4 ± 2.72% after 24 h, respectively. When the penetration of ibuprofen through the skin was evaluated, it was found that the E2 formulation increased penetration due to its lipid and nanoparticle structure. As a result of these findings, it can be said that the NLC-based gel formulation will increase the therapeutic efficacy and will be a good alternative transdermal formulation.

Graphical Abstract

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CiteScore
7.20
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