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目的考察微针阵列对纳米粒经皮给药的促渗作用,以及纳米粒在接收液和皮肤中的分布。方法采用双荧光探针指示纳米粒的经皮过程,采用Franz扩散池法,将裸鼠皮肤置于扩散池间,微针组供给室加入纳米粒混悬液,皮肤采用微针阵列作用;对照组皮肤无微针作用。采用共聚焦显微镜观察纳米粒在皮肤内的渗透过程,采用HPLC法测定纳米粒的分布。结果共聚焦显微镜观察显示纳米粒经由微针作用皮肤后产生的微孔渗透进入皮肤。48h后测定显示没有纳米粒进入接收液,皮肤中纳米粒的滞留量如下:微针组表皮125.99μg/cm2,真皮55.31μg/cm2,皮肤中总量181.30μg/cm2;对照组表皮42.15μg/cm2,真皮32.76μg/cm2,皮肤中总量74.91μg/cm2。微针可以增加纳米粒在皮肤内的滞留量(P<0.01),并且纳米粒在表皮层中的滞留量大于真皮层(P<0.01)。结论微针作用于皮肤后可显著增加纳米粒的皮肤内递送量,纳米粒沉积在皮肤中缓慢释放药物,有利于局部皮肤给药。
Objective To investigate the effect of microneedle array on transdermal delivery of nanoparticles and the distribution of nanoparticles in the receiving fluid and skin. Methods The double fluorescent probe was used to indicate the transdermal process of the nanoparticles. The Franz diffusion cell method was used. The nude mice skin was placed in the diffusion cell. The microneedle group was supplied with nanoparticle suspension and the skin was treated with microneedle array. No skin effect of microneedles. The confocal microscopy was used to observe the infiltration process of the nanoparticles in the skin and the distribution of the nanoparticles was determined by HPLC. Results Confocal microscopy showed that the nanoparticle penetrated into the skin through the micro-pores generated by the microneedles. After 48h, no nanoparticle was found in the receiving solution. The retention of nanoparticles in the skin was as follows: the microneedles epidermis 125.99μg / cm2, the dermis 55.31μg / cm2, the skin 181.30μg / cm2; the control epidermis 42.15μg / cm2, 32.76 μg / cm2 for dermis, and 74.91 μg / cm2 for skin. The microneedles could increase the retention of nanoparticles in the skin (P <0.01), and the retention of nanoparticles in the epidermis was larger than that in the dermis (P <0.01). Conclusion The microneedles can significantly increase the intradermal delivery of nanoparticles after the application of the microneedles to the skin. The deposition of the nanoparticles slowly releases the drug in the skin, which is beneficial to the local skin administration.