College of Pharmacy and Pharmaceutical Sciences, The University of Toledo Health Science Campus, The University of Toledo, Toledo, OH 43614, USA.
College of Pharmacy and Pharmaceutical Sciences, The University of Toledo Health Science Campus, The University of Toledo, Toledo, OH 43614, USA; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Ajman University, Ajman, United Arab Emirates.
Int J Pharm. 2020 Apr 30;580:119229. doi: 10.1016/j.ijpharm.2020.119229. Epub 2020 Mar 14.
The study aims to assess the ultrasound-assisted econazole nitrate (EN) permeation from topically applied formulations with potential for treating Raynaud's phenomenon. Optimization of ultrasound parameters such as the distance of the horn, application time and amplitude were performed. In vitro percutaneous absorption studies were performed using econazole formulations (F2_HPMC dispersion, F4_Lipoderm® Activemax™ Cream) across the ultrasound-treated porcine skin and were compared with the control group (skin samples without ultrasound). Histology and ATR-FTIR studies were performed on treated skin samples. A constant frequency (20 kHz) ultrasound application with 40% amplitude, 0.5 cm distance between ultrasound horn and the skin surface for 2 min was optimized. The permeation of EN was found to be higher from ultrasound-treated skin samples than the control group. Drug permeation from F2_HPMC dispersion was found to be higher as compared to the other formulations and the marketed EN cream. Histological evaluation confirmed that F2_HPMC dispersion showed no signs of toxicity. ATR-FTIR studies revealed a slight increase in the CH stretching vibrations (~2920 cm and 2850 cm) in ultrasound-treated skin samples as compared with the control. In conclusion, the ultrasound-assisted transdermal delivery of F2_HPMC dispersion could be further studied as a new therapy for Raynaud's phenomenon.
本研究旨在评估硝酸益康唑（EN）经皮透过应用制剂的超声辅助传递，这些制剂具有治疗雷诺现象的潜力。对超声参数（如喇叭距离、应用时间和振幅）进行了优化。采用超声处理的猪皮进行了体外经皮吸收研究，比较了超声处理组和对照组（未超声处理的皮肤样本）的经皮吸收情况。对处理后的皮肤样本进行了组织学和 ATR-FTIR 研究。优化后的超声参数为：固定频率（20 kHz），40%的振幅，超声喇叭与皮肤表面的距离为 0.5 cm，作用时间为 2 分钟。研究发现，与对照组相比，经超声处理的皮肤样本中 EN 的渗透量更高。与其他制剂和市售的 EN 乳膏相比，F2_HPMC 分散体的药物渗透量更高。组织学评估证实 F2_HPMC 分散体没有毒性迹象。ATR-FTIR 研究显示，与对照组相比，超声处理后的皮肤样本中的 CH 伸缩振动略有增加（~2920 cm 和 2850 cm）。总之，F2_HPMC 分散体的超声辅助经皮传递可进一步作为治疗雷诺现象的新疗法进行研究。
