Shakeel Faiyaz, Baboota Sanjula, Ahuja Alka, Ali Javed, Aqil Mohammed, Shafiq Sheikh
Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi - 110062, India.
AAPS PharmSciTech. 2007 Dec 14;8(4):E104. doi: 10.1208/pt0804104.
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, 5% wt/wt of Triacetin, 35.33% wt/wt of Tween 80, 17.66% wt/wt of Transcutol P, and 32% wt/wt of distilled water. The anti-inflammatory effects of formulation F1 showed a significant increase (P < .05) in percent inhibition value after 24 hours when compared with aceclofenac conventional gel and nanoemulsion gel on carrageenan-induced paw edema in rats. These results suggested that nanoemulsions are potential vehicles for improved transdermal delivery of aceclofenac.
本研究的目的是探究纳米乳剂制剂用于双氯芬酸经皮给药的潜力。采用自发乳化法制备了各种水包油纳米乳剂。通过构建伪三元相图确定纳米乳剂区域。对制备的纳米乳剂进行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剂制剂进行粘度、液滴大小、透射电子显微镜和折射率表征。采用Franz扩散池测定双氯芬酸经大鼠腹部皮肤的透皮渗透。将优化制剂的体外皮肤渗透曲线与双氯芬酸传统凝胶和纳米乳剂凝胶的进行比较。在优化的纳米乳剂制剂F1中观察到渗透率参数如稳态通量（J(ss)）、渗透系数（K(p)）和增强比（E(r)）显著增加，该制剂由2%（重量/重量）的双氯芬酸、10%（重量/重量）的Labrafil、5%（重量/重量）的三醋精、35.33%（重量/重量）的吐温80、17.66%（重量/重量）的Transcutol P和32%（重量/重量）的蒸馏水组成。与双氯芬酸传统凝胶和纳米乳剂凝胶相比，制剂F1对大鼠角叉菜胶诱导的爪肿胀的抗炎作用在24小时后抑制率百分比显著增加（P < 0.05）。这些结果表明纳米乳剂是改善双氯芬酸经皮给药的潜在载体。
