Department of Pharmaceutical Technology, College of Pharmacy, University of Tanta, Tanta, Egypt.
Saudi Pharm J. 2015 Jan;23(1):67-74. doi: 10.1016/j.jsps.2014.05.001. Epub 2014 May 12.
The aim of this work is to investigate penetration enhancers in proniosomes as a transdermal delivery system for nisoldipine. This was performed with the goal of optimising the composition of proniosomes as transdermal drug delivery systems. Plain proniosomes comprising sorbitan monostearate, cholesterol, ethanol and a small quantity of water were initially prepared. Subsequently, proniosomes containing lecithin or skin penetration enhancers were prepared and evaluated for transdermal delivery of nisoldipine. The plain proniosomes significantly enhanced the transdermal flux of nisoldipine to reach 12.18 μg cm(-2) h(-1) compared with a saturated aqueous drug solution which delivered the drug at a rate of 0.46 μg cm(-2) h(-1). Incorporation of lecithin into such proniosomes increased the drug flux to reach a value of 28.51 μg cm(-2) h(-1). This increase can be attributed to the penetration enhancing effect of lecithin fatty acid components. Replacing lecithin oleic acid (OA) produced proniosomes of comparable efficacy to the lecithin containing system. The transdermal drug flux increased further after incorporation of propylene glycol into the OA based proniosomes. Similarly, incorporation of isopropyl myristate into plain proniosomes increased drug flux. The study introduced enhanced proniosomes as a promising transdermal delivery carrier and highlighted the role of penetration enhancing mechanisms in enhanced proniosomal skin delivery. The study opened the way for another line of optimisation of niosome proconcentrates.
本工作旨在研究尼索地平经皮传递系统中诺米欧体中的渗透增强剂。其目的是优化诺米欧体作为经皮药物传递系统的组成。最初制备了包含山梨糖醇单硬脂酸酯、胆固醇、乙醇和少量水的普通诺米欧体。随后,制备了包含卵磷脂或皮肤渗透增强剂的诺米欧体,并评估其对尼索地平的经皮传递。与仅含药物的饱和水溶液(药物传递速率为 0.46μg·cm-2·h-1)相比,普通诺米欧体显著增强了尼索地平的经皮通量,达到 12.18μg·cm-2·h-1。将卵磷脂掺入此类诺米欧体中可增加药物通量,达到 28.51μg·cm-2·h-1。这种增加可以归因于卵磷脂脂肪酸成分的渗透增强作用。用油酸(OA)代替卵磷脂可产生与含卵磷脂系统相当功效的诺米欧体。将丙二醇掺入基于 OA 的诺米欧体中后,经皮药物通量进一步增加。同样,将肉豆蔻酸异丙酯掺入普通诺米欧体中也可增加药物通量。该研究将增强型诺米欧体引入为一种有前途的经皮传递载体,并强调了渗透增强机制在增强型诺米欧体皮肤传递中的作用。该研究为进一步优化尼索醇前浓缩物开辟了道路。