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塞来昔布经皮给药新型纳米乳剂配方的设计、开发与评价

Design, development and evaluation of novel nanoemulsion formulations for transdermal potential of celecoxib.

作者信息

Baboota Sanjula, Shakeel Faiyaz, Ahuja Alka, Ali Javed, Shafiq Sheikh

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi-110062, India.

出版信息

Acta Pharm. 2007 Sep;57(3):315-32. doi: 10.2478/v10007-007-0025-5.

DOI:10.2478/v10007-007-0025-5
PMID:17878111
Abstract

The aim of the present study was to investigate the potential of nanoemulsion formulations for transdermal delivery of celecoxib (CXB). The in vitro skin permeation profile of optimized formulations was compared with CXB gel and nanoemulsion gel. Significant increase in the steady state flux (Jss), permeability coefficient (Kp) and enhancement ratio (Er) was observed in nanoemulsion formulations T1 and T2 (p < 0.05). The highest value of these permeability parameters was obtained in formulation T2, which consisted of 2% (m/m) of CXB, 10% (m/m) of oil phase (Sefsol 218 and Triacetin), 50% (m/m) of surfactant mixture (Tween-80 and Transcutol-P) and 40% (m/m) water. The anti-inflammatory effects of formulation T2 showed a significant increase (p < 0.05) in inhibition after 24 h compared to CXB gel and nanoemulsion gel on carrageenan-induced paw edema in rats. These results suggested that nanoemulsions are potential vehicles for improved transdermal delivery of CXB.

摘要

本研究的目的是研究纳米乳剂配方用于塞来昔布(CXB)经皮给药的潜力。将优化配方的体外皮肤渗透曲线与CXB凝胶和纳米乳剂凝胶进行比较。在纳米乳剂配方T1和T2中观察到稳态通量(Jss)、渗透系数(Kp)和增强比(Er)显著增加(p < 0.05)。这些渗透参数的最高值在配方T2中获得,该配方由2%(m/m)的CXB、10%(m/m)的油相(Sefsol 218和三醋精)、50%(m/m)的表面活性剂混合物(吐温80和肉豆蔻酸异丙酯)和40%(m/m)的水组成。与CXB凝胶和纳米乳剂凝胶相比,配方T2对大鼠角叉菜胶诱导的爪肿胀的抗炎作用在24小时后抑制作用显著增加(p < 0.05)。这些结果表明,纳米乳剂是改善CXB经皮给药的潜在载体。

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