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负载特比萘芬的黄芩汤自组装纳米粒的透皮吸收评价
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| 篇名： | 负载特比萘芬的黄芩汤自组装纳米粒的透皮吸收评价 |
| TITLE： | Evaluation of transdermal absorption of self-assembled nanoparticles of Huangqin decoction loaded with terbinafine |
| 摘要： | 目的 考察负载特比萘芬（TBF）的黄芩汤（HQD）自组装纳米粒（SAN）的共载药纳米粒（TBF-HQD-SANNPs）对TBF透皮吸收的影响。方法采用高速离心结合透析法分离HQD-SAN，再通过超声-磁力搅拌法负载TBF得到TBF-HQD-SANNPs。表征该纳米粒的粒径分布、Zeta电位、多分散系数（PDI），并测定TBF的包封率（EE）与载药量（DL）。采用大鼠体外与在体透皮实验，对比分析TBF-HQD-SANNPs与TBF原料药、TBF与HQD-SAN物理混合物（TBF-HQD-SANPM）的透皮性能差异。结果TBF-HQD-SANNPs呈球形，粒径为（177.60±2.57）nm，PDI为0.1974±0.0079，Zeta电位为（－14.63±0.85）mV；TBF的EE为（99.49±0.71）%，DL为（3.22±0.10）%。体外透皮实验显示，与TBF原料药比较，TBF-HQD-SANNPs的稳态透皮速率（Jss）和皮肤滞留量分别增加至3.34倍和27.56倍（P＜0.05）；与TBF-HQD-SANPM比较，TBF-HQD-SANNPs的Jss和皮肤滞留量亦分别提高至2.04倍和7.44倍（P＜0.05）。在体透皮实验中，TBF-HQD-SANNPs的皮肤药-时曲线下面积、皮肤峰浓度较TBF原料药分别提高至2.13倍和2.06倍，较TBF-HQD-SANPM分别提高至1.59倍和1.65倍（P＜0.05）。结论TBF-HQD-SANNPs可显著提升TBF的体内外透皮吸收效率与皮肤滞留量。 |
| ABSTRACT： | OBJECTIVE To investigate the effect of Huangqin decoction （HQD）-based self-assembled nanoparticles （SAN） co-loaded with terbinafine （TBF） （TBF-HQD-SAN NPs） on the transdermal absorption of TBF. METHODS High-speed centrifugation combined with dialysis was used to separate HQD-SAN， and TBF-HQD-SAN NPs were obtained by loading TBF using the ultrasound magnetic stirring method； the particle size distribution， Zeta potential and polydispersity index （PDI） of the nanoparticle were characterized， and the encapsulation efficiency （EE） and drug loading （DL） of TBF were determined； using in vitro and in vivo transdermal experiments， the differences in transdermal performance between TBF-HQD-SAN NPs and TBF raw materials， as well as TBF and HQD-SAN physical mixture （TBF-HQD-SAN PM）， were compared and analyzed. RESULTS TBF- HQD-SAN NPs were spherical with a particle size of （177.60±2.57） nm， a PDI of 0.197 4±0.007 9， and a Zeta potential of （－14.63±0.85） mV. The EE and DL of TBF were （99.49±0.71）% and （3.22±0.10）% ， respectively. In vitro transdermal experiments， compared with TBF raw materials， the steady-state permeation rate （Jss） and skin retention of TBF-HQD-SAN NPs increased by 3.34 times and 27.56 times， respectively （P＜0.05）； compared with TBF-HQD-SAN PM， its Jss and skinretention were increased by 2.04 times and 7.44 times， respectively （P＜0.05）. In vivo transdermal experiments 69号） showed that， the area under the drug-time curve and the maximum concentration of TBF-HQD-SAN NPs increased by 2.13 times and 2.06 times respectively compared to TBF raw materials， and increased by 1.59 times and 1.65 times respectively compared to TBF-HQD-SAN PM （P＜0.05）. CONCLUSIONS TBF-HQD-SAN NPs can significantly enhance the in vitro and in vivo transdermal absorption efficiency and skin retention of TBF. |
| 期刊： | 2026年第37卷第02期 |
| 作者： | 沈成英；何沂灿；程晓；杜超颖；闵红燕；申宝德；童凌斐 |
| AUTHORS： | SHEN Chengying，HE Yican，CHENG Xiao，DU Chaoying，MIN Hongyan，SHEN Baode，TONG Lingfei |
| 关键字： | 特比萘芬；黄芩汤；自组装纳米粒；透皮吸收；皮肤滞留量；皮肤癣菌病 |
| KEYWORDS： | terbinafine； Huangqin decoction； self-assembled nanoparticles； transdermal absorption； skin retention； |
| 阅读数： | 3 次 |
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