Mansoura University, Mansoura, Egypt.
Pharm Dev Technol. 2011 Apr;16(2):93-101. doi: 10.3109/10837450903499358. Epub 2010 Jan 25.
The objective of this study was to evaluate the effect of formulation composition and continuous ultrasound at 1.5 W/Cm² intensity on the permeation of ibuprofen across polymeric and biological barriers. In vitro studies were performed using cellulose membrane and rabbit skin, whereas in vivo studies were performed on rabbits. Overall, higher transport data were obtained with the cellulose membrane. Nonetheless, with both barriers, transport was higher with the gel formulation than oleaginous or emulsion based preparations, which was also dependent on the viscosity of the gel and the concentration of the formulation additives. Transport increased with the increase in alcohol concentration and decreased with the addition of propylene glycol. Ultrasound had a significant effect on ibuprofen transport. For example, an 11-fold increase in drug permeation across cellulose membrane was observed after the application of ultrasound. Similar effect was observed in animal studies. Ibuprofen plasma concentration increased with the concentration of the drug in the gel, which significantly increased after the application of ultrasound. It was concluded that aqueous gel formulations act as ideal coupling agents for topical application of drugs. Nonetheless, in addition to ultrasound, the composition of the gel is expected to have a significant effect on the transdermal delivery of drugs.
本研究旨在评估制剂组成和 1.5 W/cm² 强度的连续超声对布洛芬穿过聚合体和生物屏障的渗透作用的影响。体外研究采用纤维素膜和兔皮进行,体内研究则在兔子身上进行。总的来说,纤维素膜的传输数据更高。尽管如此,对于两种屏障,凝胶制剂的传输高于油性或乳剂制剂,这也取决于凝胶的粘度和制剂添加剂的浓度。随着酒精浓度的增加,传输增加,随着丙二醇的添加,传输减少。超声对布洛芬的传输有显著影响。例如,在施加超声后,观察到纤维素膜上药物渗透增加了 11 倍。在动物研究中也观察到类似的效果。布洛芬的血浆浓度随着凝胶中药物的浓度增加而增加,在施加超声后显著增加。研究结论认为,水性凝胶制剂是药物局部应用的理想偶联剂。尽管如此,除了超声之外,凝胶的组成预计也会对药物的经皮传递产生重大影响。