不同物理促透技术对芥子碱硫氰酸盐体外透皮吸收的影响

目的 比较微针、超声导入和离子导入3种物理方式促药物吸收技术对芥子碱硫氰酸盐(ST)体外透皮吸收的效果,探讨不同物理方式促进透皮吸收的规律.方法 采用改良Franz扩散池和SD大鼠腹部皮肤,分别在微针、超声导入或离子导入条件下进行透皮实验.以2 mg/ml ST水溶液为供体溶液,定时从接收池中取样,用高效液相色谱法(HPLC)测定不同时间点样品中药物含量,计算累积透过量和稳态透皮吸收速度.取各促透皮技术处理12 h后的皮肤制作病理切片,观察不同促透技术对皮肤结构的影响,探讨其促吸收机制.结果 单纯透皮条件下,ST累积透过量较少.不同促透技术对ST有较明显促透效果,排序如下:微针>超声导入>离子导入.微针在皮肤表面形成实质性孔道,促进ST透皮吸收的效果最明显.超声导入通过扰乱皮肤角质层的紧密结构促透.离子导入对皮肤结构影响较小.结论 本研究为不同透皮给药促透技术的选择提供了依据.

Effect of physical techniques on in vitro transdermal permeability of sinapine thiocyanate

Objective To compare the improvement effect of three physical techniques on the transdermal absorption of sinap?ine thiocyanate(ST)in vitro,including microneedles,sonophoresis and iontophoresis,and to evaluate the mechanism and rules of physcial techniques on the transdermal absorption of poorly transdermal absorbed drugs. Methods In vitro transdermal experiment was carried out under the circumstances of microneedles,sonophoresis or iontophoresis,using the modified Franz diffusion pool. The 2 mg/ml ST solution was adopted as the donor solution, and the SD rats′abdomen skin was used as the model skin. Sampling was car?ried out at the predetermined time points and each sample was analyzed by HPLC. Cumulative transdermal amount and steady transder?mal absorption rate were calculated. Pathological slides were made after the skins were treated with microneedles ,sonophoresis and iontophoresis for 12 h. The structure changes were observed to evaluate the transdermal improvement mechanism of different technolo?gies. Results Accumulated transdermal amount of ST was little without any techniques. The transdermal improvement effect of differ?ent technologies was as follows:microneedles>sonophoresis>iontophoresis. A substantial hole formed on the skin by microneedles to promote ST transdermal absorption obviously. Sonophoresis disrupted the tight structure of skin and improved the transdermal absorp?tion of drugs easily. The effect of iontophresis on skin structure was little. Conclusion This study provides experimental evidence for choice of different techniques to improve transdermal absorption.