1.江西省人民医院(南昌医学院第一附属医院)药学部,南昌;330006
2.成都中医药大学药学院,成都 611137
3.江西中医药大学现代中药制剂教育部重点实验室,南昌 330004
4.南昌医学院药学院,南昌 330052
Received:01 November 2025,
Revised:2025-11-19,
Accepted:31 December 2025,
Published:30 January 2026
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沈成英,何沂灿,程晓,等.负载特比萘芬的黄芩汤自组装纳米粒的透皮吸收评价[J].中国药房,2026,37(02):180-185.
SHEN Chengying,HE Yican,CHENG Xiao,et al.Evaluation of transdermal absorption of self-assembled nanoparticles of Huangqin decoction loaded with terbinafine[J].ZHONGGUO YAOFANG,2026,37(02):180-185.
沈成英,何沂灿,程晓,等.负载特比萘芬的黄芩汤自组装纳米粒的透皮吸收评价[J].中国药房,2026,37(02):180-185. DOI: 10.6039/j.issn.1001-0408.2026.02.08.
SHEN Chengying,HE Yican,CHENG Xiao,et al.Evaluation of transdermal absorption of self-assembled nanoparticles of Huangqin decoction loaded with terbinafine[J].ZHONGGUO YAOFANG,2026,37(02):180-185. DOI: 10.6039/j.issn.1001-0408.2026.02.08.
目的
2
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-SAN NPs)对TBF透皮吸收的影响。
方法
2
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-SAN NPs。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-SAN NPs与TBF原料药、TBF与HQD-SAN物理混合物(TBF-HQD-SAN PM)的透皮性能差异。
结果
2
TBF-HQD-SAN NPs呈球形,粒径为(177.60±2.57)nm,PDI为0.197 4±0.007 9,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-SAN NPs的稳态透皮速率(
J
ss
)和皮肤滞留量分别增加至3.34倍和27.56倍(
P
<0.05);与TBF-HQD-SAN PM比较,TBF-HQD-SAN NPs的
J
ss
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-SAN NPs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-SAN PM分别提高至1.59倍和1.65倍(
P
<0.05)。
结论
2
TBF-HQD-SAN NPs可显著提升TBF的体内外透皮吸收效率与皮肤滞留量。
OBJECTIVE
2
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
2
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
2
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 (
J
ss
) 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
J
ss
and skin retention were increased by 2.04 times and 7.44 times, respectively (
P
<0.05).
In vivo
transdermal experiments 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
2
TBF-HQD-SAN NPs can significantly enhance the
in vitro
and
in vivo
transdermal absorption efficiency and skin retention of TBF.
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