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采用回流法制备黄柏提取物,再制成o/w型乳膏.用HPLC法测定盐酸小檗碱的含量.以离体裸鼠皮肤为屏障,用改良Franz扩散池法考察乳膏中盐酸小檗碱的体外透皮性能,探讨滚轮微针技术对黄柏提取物乳膏中盐酸小檗碱体外经皮渗透行为和皮肤滞留量的影响.结果显示,不用或采用微针处理组乳膏中盐酸小檗碱12h的累积渗透量为(0.161±0.008)、(0.978±0.034) mg/cm2,经皮渗透速率为(0.035±0.007)、(0.197±0.018) mg·cm-2·h-1,皮肤滞留量为(0.373±0.021)、(1.364±0.342)mg/cm2.可见,滚轮微针技术能显著提高外用黄柏提取物乳膏中盐酸小檗碱的经皮渗透量(P<0.05),增加皮肤内药物滞留量(P<0.05).  相似文献
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Many chronic wounds exhibit high matrix metalloproteinase (MMP) activity that impedes the normal wound healing process. Intradermal delivery (IDD) of sub-antimicrobial concentrations of doxycycline, as an MMP inhibitor, could target early stages of chronic wound development and inhibit further wound progression. To deliver doxycycline intradermally, the skin barrier must be disrupted. Microneedle rollers offer a minimally invasive technique to penetrate the skin by creating multiple microchannels that act as temporary conduits for drugs to diffuse through. In this study, an innovative and facile approach for delivery of doxycycline across Strat-MTM membrane was investigated using microneedle rollers. The quantity and rate of doxycycline diffusing through the micropores directly correlated with increasing microneedle lengths (250, 500 and 750 μm). Treatment of Strat-MTM with microneedle rollers resulted in a reduction in fibroblast-mediated collagen gel contraction and MMP activity compared with untreated Strat-MTM. Our results show that treatment of an epidermal mimetic with microneedle rollers provides sufficient permeabilization for doxycycline diffusion and inhibition of MMP activity. We conclude that microneedle rollers are a promising, clinically ready tool suitable for delivery of doxycycline intradermally to treat chronic wounds.  相似文献
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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、12h取接收液0.2ml,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。  相似文献
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