Effect of different density microneedle-roller on transdermal delivery of triamcinolone acetonide
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摘要: 目的 探讨不同密度滚轮微针对曲安奈德经皮渗透的影响。 方法 采用改良Franz扩散池法考察体外经皮渗透特性,以离体裸鼠皮肤为屏障,对照组、192针、540针滚轮微针处理组分别于2、4、6、8、10、12 h取接收液0.2 ml,用HPLC法测定曲安奈德含量,计算累积渗透量,并测定皮肤内曲安奈德滞留量。采用测定血药浓度法考察在体吸收特性,在体给药2h后HPLC法测定各组皮肤及血浆中曲安奈德的含量。 结果 两种密度滚轮微针对曲安奈德均有不同程度的促透作用。离体透皮实验结果显示,192针微针处理组和540针微针处理组的累积渗透量Q分别是对照组的1.3倍和2.2倍,相应的皮肤内滞留量也分别是对照组的1.9倍和2.8倍。在体实验结果显示,192针微针和540针微针组的皮肤滞留量是对照组的2.1和2.3倍,同时也将血药浓度提高了1.3倍和1.4倍。 结论 两种不同密度滚轮微针均能有效提高曲安奈德的经皮渗透量,提高皮肤内药物含量,同时也导致血药浓度的增加,且不同密度微针的促透作用有所不同。Abstract: Objective To study the effects of different density microneedle-roller arrays on transdermal delivery of triamcinolone acetonide. Methods The in vitro permeation characteristics through isolated nude mouse skin were studied by modified Franz diffusion cells. Levels in the receptor solution of the control group, the 192 needles microneedle rooler group and the 540 needles microneedle rooler group were measured by HPLC at 2、4、6、8、10 and 12 h, and sampling volume was 0.2 ml. The accumulative penetration amount were counted and the level of triamcinolone acetonide in skin were determined. Plasma concentrations of triamcinolone acetonide and skin volume were measured 2 hours later after administration by HPLC to observe the penetration of triamcinolone acetonide in vivo. Results Different density microneedle-roller could promote the transdermal delivery of triamcinolone acetonide respectively. Transdermal experiment results showed that the cumulative infiltration volume of 192 needles group was about 1.3 times of the control samples, and 540 needles was 2.2 times. Accordingly, skin retention volume were1.9times and 2.8 times of the control group respectively. In vivo results showed that skin retention volume were 2.1 times and 2.3 times of control group, while triamcinolone acetonide in plasma were 1.3 times and 1.4 times of control group. Conclusion Microneedles could effectively promote the skin permeability and deposition of triamcinolone acetonide, and triamcinolone acetonide in plasma was increased at the same time. The promoting of different density was diverse.
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Key words:
- microneedle-roller /
- triamcinolone acetonide /
- percutaneous penetration
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