Nanoemulsions as Vehicles for Transdermal Delivery of Aceclofenac
Nanoemulsions as Vehicles for Transdermal Delivery of Aceclofenac
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DOI：
10.1208/pt0804104
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发表时间：
2007-10-01
影响因子：
3.3
通讯作者：
Shafiq, Sheikh
中科院分区：
文献类型：
--
作者：
Shakeel, Faiyaz;Baboota, Sanjula;Shafiq, Sheikh
本研究的目的是研究醋氯芬酸纳米乳剂经皮给药的可能性。采用自发乳化法制备了不同的水包油纳米乳液。通过构建拟三元相图确定了纳米乳状液的区域。对制备的纳米乳液进行了不同的热力学稳定性测试。对通过热力学稳定性测试的纳米乳液配方进行了粘度、液滴大小、透射电子显微镜和折射率的表征。用Franz扩散池测定醋氯芬酸对大鼠腹部皮肤的透皮吸收。并与醋氯芬酸常规凝胶和纳米乳凝胶剂的体外透皮吸收情况进行了比较。以醋氯芬酸2%wt/wt、拉布拉非10%wt/wt、三乙酸三乙酯5%wt/wt、吐温80(R)35.33%wt/wt、Transcutol P(R)17.66%wt/wt和蒸馏水32%wt/wt组成的优化纳米乳剂F1的渗透系数(J(Ss))、渗透系数(K-p)和增透比(E-r)均有显著提高。方剂F1的抗炎作用明显增强(P
The aim of the present study was to investigate the potential of a nanoemulsion formulation for transdermal delivery of aceclofenac. Various oil-in-water nanoemulsions were prepared by the spontaneous emulsification method. The nanoemulsion area was identified by constructing pseudoternary phase diagrams. The prepared nanoemulsions were subjected to different thermodynamic stability tests. The nanoemulsion formulations that passed thermodynamic stability tests were characterized for viscosity, droplet size, transmission electron microscopy, and refractive index. Transdermal permeation of aceclofenac through rat abdominal skin was determined by Franz diffusion cell. The in vitro skin permeation profile of optimized formulations was compared with that of aceclofenac conventional gel and nanoemulsion gel. A significant increase in permeability parameters such as steady-state flux (J(ss)), permeability coefficient (K-p), and enhancement ratio (E-r) was observed in optimized nanoemulsion formulation F1, which consisted of 2% wt/wt of aceclofenac, 10% wt/wt of Labrafil (R), 5% wt/wt of Triacetin (R), 35.33% wt/wt of Tween 80 (R), 17.66% wt/wt of Transcutol P (R), and 32% wt/wt of distilled water. The anti-inflammatory effects of formulation F1 showed a significant increase (P