Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), M. B. Road, New Delhi 110062, India.
Int J Biol Macromol. 2014 Mar;64:144-9. doi: 10.1016/j.ijbiomac.2013.11.018. Epub 2013 Dec 1.
The purpose of this work was to develop a transdermal gel formulation for enhanced delivery of valsartan for the management of hypertension. Transdermal gels bearing valsartan, carbopol and 1,8-cineole (penetration enhancer) were prepared and characterized for various parameters including in vitro skin permeation studies, pH, spreadability, viscosity, skin irritation potential and in vivo antihypertensive activity. Optimized valsartan gel formulation (VTGF9) showed highest transdermal flux (143.51 μg/cm(2)/h), with an enhancement ratio of 4.53 when compared to control gel formulation (VTGF8). Incorporation of 1,8-cineole and ethanol in gel formulation enhance the permeation of valsartan significantly. Skin irritation and histopathological study revealed that the VTGF9 was safe, less irritant and well tolerable formulation for transdermal delivery. In vivo antihypertensive activity revealed that optimized VTGF9 was successful in reverting the rat BP to normal values in experimental hypertensive rats. Finally, it could be concluded that VTGF9 accentuates the flux of valsartan and is an efficient transdermal therapeutic system for delivery of valsartan.
本工作旨在开发一种用于增强缬沙坦传递的透皮凝胶制剂，以用于治疗高血压。制备了含有缬沙坦、卡波姆和 1,8-桉叶油醇（渗透促进剂）的透皮凝胶，并对各种参数进行了表征，包括体外皮肤渗透研究、pH 值、铺展性、粘度、皮肤刺激性潜力和体内降压活性。与对照凝胶制剂（VTGF8）相比，优化的缬沙坦凝胶制剂（VTGF9）显示出最高的透皮通量（143.51μg/cm²/h），增强比为 4.53。凝胶制剂中加入 1,8-桉叶油醇和乙醇可显著增强缬沙坦的渗透。皮肤刺激性和组织病理学研究表明，VTGF9 是一种安全、刺激性较小且可耐受的透皮给药制剂。体内降压活性研究表明，优化后的 VTGF9 成功地将实验性高血压大鼠的血压恢复到正常水平。综上所述，VTGF9 可增强缬沙坦的通量，是一种有效的缬沙坦透皮治疗系统。
