Huang Bin, Dong Wei-Jiang, Yang Gao-Yi, Wang Wei, Ji Cong-Hua, Zhou Fei-Ni
Department of Ultrasound, First Affiliated Hospital of Zhejiang Chinese Medical University, Hangzhou, People's Republic of China.
Department of Ultrasonography, Tongxiang Chinese Medicine Hospital, Jiaxing, People's Republic of China.
Drug Des Devel Ther. 2015 Jul 23;9:3867-76. doi: 10.2147/DDDT.S75702. eCollection 2015.
The purpose of the present study was to develop a novel transdermal drug-delivery system comprising a polyamidoamine dendrimer coupled with sonophoresis to enhance the permeation of diclofenac (DF) through the skin. The novel transdermal drug-delivery system was developed by using a statistical Plackett-Burman design. Hairless male Wistar rat skin was used for the DF-permeation study. Coupling media concentration, ultrasound-application time, duty cycle, distance from probe to skin, and a third-generation polyamidoamine-dendrimer concentration were selected as independent variables, while in vitro drug release was selected as a dependent variable. Independent variables were found to be statistically significant (P<0.05). DF gel without dendrimer and ultrasound treatment to skin (passive delivery, run 13) showed 56.69 µg/cm(2) cumulative drug permeated through the skin, while the DF-dendrimer gel without sonophoresis treatment (run 14) showed 257.3 µg/cm(2) cumulative drug permeated through the skin after 24 hours. However, when the same gel was applied to sonophoresis-treated skin, drastic permeation enhancement was observed. In the case of run 3, the cumulative drug that permeated through the skin was 935.21 µg/cm(2). It was concluded that dendrimer-coupled sonophoresis-mediated transdermal drug delivery system has the potential to enhance the permeation of DF through the skin.
本研究的目的是开发一种新型透皮给药系统，该系统由聚酰胺胺树枝状大分子与超声导入技术相结合，以增强双氯芬酸（DF）透过皮肤的渗透。采用统计的Plackett-Burman设计开发了新型透皮给药系统。选用无毛雄性Wistar大鼠皮肤进行DF渗透研究。选择耦合介质浓度、超声作用时间、占空比、探头与皮肤的距离以及第三代聚酰胺胺树枝状大分子浓度作为自变量，而体外药物释放作为因变量。发现自变量具有统计学意义（P<0.05）。未添加树枝状大分子且未对皮肤进行超声处理的DF凝胶（被动给药，第13次试验）显示，有56.69μg/cm²的药物累积透过皮肤，而未进行超声导入处理的DF树枝状大分子凝胶（第14次试验）在24小时后显示有257.3μg/cm²的药物累积透过皮肤。然而，当将相同的凝胶应用于经超声导入处理的皮肤时，观察到显著的渗透增强。在第3次试验中，透过皮肤的累积药物量为935.21μg/cm²。得出的结论是，树枝状大分子耦合超声导入介导的透皮给药系统有潜力增强DF透过皮肤的渗透。
