Zeyu Wang,Daiyan Zhang,Mingju Shui,Ian Wa Ho,Weng Si Kou,Jianwen Wei,Jian-Bo Wan,Ruibing Wang,Qing-Wen Zhang
Background Ginsenoside, as an active ingredient in traditional Chinese medicine, has been widely used for skin whitening for several years. Recent research has found that Panax notoginseng has a higher content of ginsenosides compared with the Panax ginseng. Those ginsenosides have promising potential to be developed as skin whitening agents. Methods We selected five dammarane ginsenosides isolated from P. notoginseng and their mixtures to investigate the skin lightning activity. Zebrafish embryo model was used for initial screening of the whitening activity. Subsequently, the whitening effect of components was examined and compared via testing the inhibition of melanin and activity of tyrosinase in B16 cells treated with these components. Molecular docking was also applied to investigate the interactions between ginsenosides and tyrosinase. Finally, the most effective saponins were selected for dosage form optimization and the whitening effect of saponin-loaded ethosomes was further demonstrated on the C57BL/6 mouse model. Results Experimental results showed that the protopanaxtriol saponins (PTS) were the most potent saponins with a decent safety profile, and the molecule docking results demonstrated that PTS had strong inhibitory ability to tyrosinase. PTS was successfully encapsulated into ethosomes with an encapsulation efficiency of 93%. The PTS ethosome gel could effectively inhibit the melanin production caused by UVB tanning on the back skin of mice. Conclusion The PTS ethosome gel provides an effective and safe formulation of PTS to whiten the UVB-tanned skin in vivo and could be used as a potential skin whitening agent in the future.
Transdermal administration is a promising non-invasive and convenient method of drug delivery in clinic and avoid serious gastrointestinal adverse reactions. In this study, a hybrid nanocarrier was developed to facilitate transdermal delivery of drugs. The low water-soluble ketoprofen (KP) was ultrasonically loaded on functionalized multi-walled carbon nanotubes (f-MWCNTs), and the preparation process was optimized using Box-Behnken design. Then, KP-loaded f-MWCNTs composite ethosomes (f-MWCNTs-KP-ES) were prepared by a single-step injection technology. Over the study period, the preparation was verified by a series of characterizations, and ex vivo release characteristics, ex vivo permeation of rat skin and in vivo pharmacokinetics were studied. The characterization results consistently showed that f-MWCNTs-KP-ES were successfully prepared. The preparation can obviously improve the solubility of KP. Ex vivo permeation experiments showed that had a sustained release effect and the skin penetration rate of f-MWCNTs-KP-ES gel is the fastest, with a cumulative permeation amount of 602.35 ± 41.06 μg/cm 2 . In addition, both ethosomes and f-MWCNTs could increase the retention of drugs and form drug reservoirs. Fluorescence microscope images of rat skin clearly illustrated the faster and deeper penetration of f-MWCNTs composite ethosomes formulation loaded with rhodamine B (RB) (f-MWCNT-RB-ES). In vivo pharmacokinetic experiments showed the area under the drug time curve (AUC 0-t ) and elimination half-life (T 1/2β ) of f-MWCNTs-KP-ES gel group were significantly increased and prolonged compared with KP commercial gel group, respectively. The overall data indicate that the f-MWCNTs composite ethosomes formulation is a promising transdermal drug delivery system .
危险品化学品经营许可证（带存储）