School of Mechanical Engineering, Hangzhou Dianzi University, Hangzhou, 310018, China.
College of Pharmacy, Hangzhou Medical College, Hangzhou, 310014, China.
Drug Deliv Transl Res. 2024 Nov;14(11):3239-3249. doi: 10.1007/s13346-024-01547-4. Epub 2024 Feb 26.
Microneedle transdermal administration and low-frequency ultrasound represent two important physical penetration-promoting methods for enhancing drug penetration. This article aims to investigate and compare the effects of drug penetration enhancement through transdermal administration using vibrating microneedles versus low-frequency sonophoresis. In Vitro permeation studies were conducted using Valia-Chien double chamber diffusion cells to evaluate the transdermal delivery of tetramethylpyrazine hydrochloride (TMPH). The TMPH concentration in the receiving compartment was determined using high-performance liquid chromatography (HPLC). Several combinations of microneedles and ultrasound settings were investigated, including different needle heights, vibration frequencies, exposure times, and assorted distances of ultrasound horn and skin. The results revealed the vibrating microneedle system as the most efficacious treatment to increase the TMPH permeability into the rat skin. The combination of a larger needle, higher frequency, and a 3-min exposure led to a 41.92-fold increase in cumulative permeability compared to the control group. The ultrasound treatment exhibited a moderate enhancement effect on TMPH skin penetration. Using a horn-to-skin distance of 3 mm and a 3-min exposure resulted in a 4.34-fold increase in TMPH cumulative permeation compared to the control group. It could be concluded that while both the vibrating microneedle and the low-frequency ultrasound systems act as penetration enhancers for promoting the TMPH permeation through the skin, the vibrating microneedle system notably demonstrates a more effective penetration-promoting effect.
微针经皮给药和低频超声是增强药物渗透的两种重要物理渗透促进方法。本文旨在研究和比较经皮给药时使用振动微针和低频声孔法增强药物渗透的效果。采用 Valia-Chien 双室扩散池进行体外渗透研究,评估盐酸四甲基吡嗪(TMPH)的经皮传递。采用高效液相色谱法(HPLC)测定接收室中 TMPH 的浓度。研究了几种微针和超声设置的组合,包括不同的针高、振动频率、暴露时间以及超声喇叭和皮肤的不同距离。结果表明,振动微针系统是增加 TMPH 透皮进入大鼠皮肤的最有效治疗方法。较大的针、较高的频率和 3 分钟的暴露组合使累积渗透度比对照组增加了 41.92 倍。超声处理对 TMPH 皮肤渗透具有中等增强作用。使用喇叭到皮肤的距离为 3mm 和 3 分钟的暴露使 TMPH 的累积渗透度比对照组增加了 4.34 倍。可以得出结论,虽然振动微针和低频超声系统都可作为渗透增强剂促进 TMPH 通过皮肤渗透,但振动微针系统显著显示出更有效的渗透促进作用。