负载特比萘芬的黄芩汤自组装纳米粒的透皮吸收评价OA

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 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 TBF-HQD-SAN NPs can significantly enhance the in vitro and in vivo transdermal absorption efficiency and skin retention of TBF.