改装滚轮微针用于醋酸曲安奈德经皮给药的特性试验

目的:评价改装滚轮微针用于曲安奈德经皮给药的力度可控性、释药重现性和皮肤刺激性。方法:改装市售滚轮微针;石蜡切片、HE染色法观察不同微针使用力度(2.5,5.0,7.5,10.0,12.5,15.0,17.5,20.0 N)时的皮肤微孔深度,探讨改装前后其力度可控性;以离体裸鼠皮肤为屏障,Franz扩散池法考察改装前后曲安奈德经皮渗透特性;评分法测定皮肤刺激性。结果:皮肤微孔深度随微针使用力度的增加而加大,微孔深度范围由65.28~106.25 μm收窄为改装后的71.53~97.92 μm,其RSD范围由10.45%~19.69%显著下降至改装后的2.33%~9.21%。在相同微针使用力度下,曲安奈德的累积释药量RSD范围由改装前的34.75%~55.92%,显著下降至改装后的14.29%~29.73%。改装滚轮微针用药1 h时出现轻度皮肤刺激性,之后消失。结论:与市售滚轮微针相比,改装滚轮微针具有较好的力度可控性、释药重现性,以及较小的皮肤刺激性。

Characteristic test on transdermal delivery of triamcinolone acetonide by using modified microneedle roller

OBJECTIVE To study the controllability of pressure, reproducibility of drug release and skin irritation of modified microneedle roller for transdermal delivery of triamcinolone acetonide. METHODS The commercially available microneedle roller was modified. Controllability of pressure was evaluated before and after modification, and pore depths under different pressure (2.5, 5.0, 7.5, 10.0, 12.5, 15.0, 17.5 and 20.0 N) were observed by utilizing paraffin sections and HE staining method. The in vitro permeation characteristics of triamcinolone acetonide through isolated nude mouse skin were studied by Franz diffusion cell before and after modification. Scoring method was used to investigate the skin irritation. RESULTS The pore depth increased as pressure increased. The range of pore depth narrowed from 65.28-106.25 to 71.53-97.92 micrometers by the modified microneedle roller. The range of RSD significantly decreased from 10.45%-19.69% to 2.33%-9.21% in the modified group. At the same pressure of microneedle roller, RSD range of accumulative penetration amount of triamcinolone acetonide decreased markedly from 34.75%-55.92% to 14.29%-29.73%. The mild stimulus intensity was observed one hour after administration using modified microneedle roller, and then all irritation symptoms disappeared.CONCLUSION Compared with commercially available microneedle roller, the modified one shows better controllability of pressure, reproducibility of drug release, but less skin irritation.