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用于局部给药的右布洛芬负载型乳胶凝胶的力学性能、皮肤渗透性及体内评价

Mechanical properties, skin permeation and in vivo evaluations of dexibuprofen-loaded emulsion gel for topical delivery.

作者信息

Jin Sung Giu, Yousaf Abid Mehmood, Son Mi Woon, Jang Sun Woo, Kim Dong Wuk, Kim Jong Oh, Yong Chul Soon, Kim Jeong Hoon, Choi Han-Gon

机构信息

Pharmaceutical Product Research Laboratories, Dong-A Pharm. Co. Ltd., Yongin-Si, Kyunggi-Do, 449-905, South Korea.

出版信息

Arch Pharm Res. 2015 Feb;38(2):216-22. doi: 10.1007/s12272-014-0367-8. Epub 2014 Mar 24.

Abstract

The aim of this research was to evaluate the gel properties, skin permeation and in vivo drug efficacy of a novel dexibuprofen-loaded emulsion gel for topical delivery. In this study, the dexibuprofen-loaded emulsion gel and ibuprofen-loaded emulsion gel were prepared with isopropanol, Tween 80, propylene glycol, isopropyl myristate and carbopol. Their mechanical properties such as hardness and adhesiveness were assessed. Moreover, their skin permeation, anti-inflammatory and anti-nociceptive efficacy were evaluated using Franz diffusion cell with the hairless mouse skin, the carrageenan-induced paw oedema test and paw pressure test in rat's hind paws compared with the commercial hydrogel, respectively. The dexibuprofen emulsion gel and ibuprofen emulsion gel provided significantly higher hardness and adhesiveness than the commercial hydrogel. The dexibuprofen emulsion gel enhanced skin permeability by about twofold and 3.5-fold without lag time compared to the ibuprofen emulsion gel and the commercial hydrogel, respectively, suggesting its faster skin permeation. Moreover, the anti-inflammatory efficacy and alleviation in carrageenan-induced inflammation was in the order of dexibuprofen emulsion gel > commercial hydrogel > ibuprofen emulsion gel. The dexibuprofen emulsion gel furnished significantly higher nociceptive thresholds than the ibuprofen emulsion gel and the commercial hydrogel, leading to the most improved anti-nociceptive efficacy. Thus, this dexibuprofen-loaded emulsion gel with good mechanical property, rapid skin permeation and excellent anti-inflammatory and anti-nociceptive efficacy would be a strong candidate for the topical delivery of anti-inflammatory dexibuprofen.

摘要

本研究旨在评估一种用于局部给药的新型载右布洛芬乳剂凝胶的凝胶特性、皮肤渗透性及体内药物疗效。在本研究中,载右布洛芬乳剂凝胶和载布洛芬乳剂凝胶由异丙醇、吐温80、丙二醇、肉豆蔻酸异丙酯和卡波姆制备而成。评估了它们的硬度和黏附性等机械性能。此外,分别使用Franz扩散池和无毛小鼠皮肤、角叉菜胶诱导的大鼠后爪足肿胀试验及爪压力试验,与市售水凝胶相比,评估了它们的皮肤渗透性、抗炎和抗伤害感受疗效。右布洛芬乳剂凝胶和布洛芬乳剂凝胶的硬度和黏附性均显著高于市售水凝胶。与布洛芬乳剂凝胶和市售水凝胶相比,右布洛芬乳剂凝胶分别使皮肤渗透率提高了约两倍和3.5倍,且无滞后时间,表明其皮肤渗透更快。此外,抗炎疗效及对角叉菜胶诱导炎症的缓解作用顺序为:右布洛芬乳剂凝胶>市售水凝胶>布洛芬乳剂凝胶。右布洛芬乳剂凝胶的伤害感受阈值显著高于布洛芬乳剂凝胶和市售水凝胶,抗伤害感受疗效改善最为明显。因此,这种具有良好机械性能、快速皮肤渗透及优异抗炎和抗伤害感受疗效的载右布洛芬乳剂凝胶有望成为局部递送抗炎药物右布洛芬的有力候选者。

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