Research Center for Pharmaceutical Nanotechnology, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Biomed Res Int. 2013;2013:616810. doi: 10.1155/2013/616810. Epub 2013 Jul 14.
The aim of this study was to improve the transdermal permeation of Diclofenac sodium, a poorly water-soluble drug, employing conventional liposomes, ethosomes, and transfersomes. The prepared formulations had been characterized for the loaded drug amount and vesicle size. The prepared vesicular systems were incorporated into 1% Carbopol 914 gel, and a survey of in vitro drug release and drug retention into rat skin has been done on them using a modified Franz diffusion cell. The cumulative amount of drug permeated after 24 h, flux, and permeability coefficient were assessed. Stability studies were performed for three months. The size of vesicles ranged from 145 to 202 nm, and the encapsulation efficiency of the Diclofenac sodium was obtained between 42.61% and 51.72%. The transfersomes and ethosomes provided a significantly higher amount of cumulative permeation, steady state flux, permeability coefficient, and residual drug into skin compared to the conventional liposomes, conventional gel, or hydroethanolic solution. The in vitro release data of all vesicular systems were well fit into Higuchi model (RSD > 0.99). Stability tests indicated that the vesicular formulations were stable over three months. Results revealed that both ethosome and transfersome formulations can act as drug reservoir in skin and extend the pharmacologic effects of Diclofenac sodium.
本研究旨在通过使用常规脂质体、醇质体和传递体来提高难溶性药物双氯芬酸钠的经皮渗透。对所制备的制剂进行了载药量和囊泡大小的特征描述。将制备的囊泡系统掺入 1%卡波姆 914 凝胶中,并使用改良的 Franz 扩散池对其进行了体外药物释放和药物在大鼠皮肤中的保留的研究。评估了 24 小时后累积渗透药物量、通量和渗透系数。进行了三个月的稳定性研究。囊泡的大小范围为 145 至 202nm,双氯芬酸钠的包封效率在 42.61%至 51.72%之间。与常规脂质体、常规凝胶或水醇溶液相比,传递体和醇质体提供了更高的累积渗透量、稳态通量、渗透系数和皮肤内残留药物。所有囊泡系统的体外释放数据均很好地符合 Higuchi 模型(RSD > 0.99)。稳定性测试表明,囊泡制剂在三个月内稳定。结果表明,醇质体和传递体制剂都可以作为皮肤中的药物储库,延长双氯芬酸钠的药效。