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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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沈成英 ,何沂灿 ,程 晓 ,杜超颖 ,闵红燕 ,申宝德 ,童凌斐 [1.江西省人民医院(南昌医学院第一附属医
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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]
中图分类号 R283.6;R943 文献标志码 A 文章编号 1001-0408(2026)02-0180-06
DOI 10.6039/j.issn.1001-0408.2026.02.08
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-SAN NPs)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-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
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(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-SAN PM 比较,TBF-HQD-SAN NPs 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-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 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。
关键词 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
Evaluation of transdermal absorption of self-assembled nanoparticles of Huangqin decoction loaded with
terbinafine
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SHEN Chengying ,HE Yican ,CHENG Xiao ,DU Chaoying ,MIN Hongyan ,SHEN Baode ,TONG Lingfei
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[1. Dept. of Pharmacy, Jiangxi Provincial People’s Hospital (the First Affiliated Hospital of Nanchang Medical
College), Nanchang 330006, China;2. School of Pharmacy, Chengdu University of Traditional Chinese
Medicine, Chengdu 611137, China;3. Key Laboratory of Modern Preparation of Traditional Chinese Medicine,
Ministry of Education, Jiangxi University of Chinese Medicine, Nanchang 330004, China;4. School of
Pharmacy, Nanchang Medical College, Nanchang 330052, China]
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<
Δ 基金项目 江西省自然科学基金青年项目(No.20232BAB2161- 0.05); compared with TBF-HQD-SAN PM, its Jss and skin
24);江西省卫生健康委科技计划资助项目(No.202510005);赣鄱俊才 retention were increased by 2.04 times and 7.44 times,
支持计划·高层次高技能领军人才培养项目(No. 赣人社字〔2024〕 respectively (P<0.05). In vivo transdermal experiments
69号) showed that, the area under the drug-time curve and the
*第一作者 副主任中药师,副教授,博士。研究方向:中药纳米给
maximum concentration of TBF-HQD-SAN NPs increased by
药系统。E-mail:984075899@qq.com
# 通信作者 副 主 任 药 师 。 研 究 方 向 :医 院 药 学 。 E-mail: 2.13 times and 2.06 times respectively compared to TBF raw
15870637696@126.com materials, and increased by 1.59 times and 1.65 times
· 180 · China Pharmacy 2026 Vol. 37 No. 2 中国药房 2026年第37卷第2期

