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Microemulsion-based hydrogels for enhancing epidermal/dermal deposition of topically administered 20(S)-protopanaxadiol: in vitro and in vivo evaluation studies.


ABSTRACT:

Background

20(S)-Protopanaxadiol (20S-PPD) is a fully deglycosylated ginsenoside metabolite and has potent dermal antiaging activity. However, because of its low aqueous solubility and large molecular size, a suitable formulation strategy is required to improve its solubility and skin permeability, thereby enhancing its skin deposition. Thus, we optimized microemulsion (ME)-based hydrogel (MEH) formulations for the topical delivery of 20S-PPD.

Methods

MEs and MEHs were formulated and evaluated for their particle size distribution, morphology, drug loading capacity, and stability. Then, the deposition profiles of the selected 20S-PPD-loaded MEH formulation were studied using a hairless mouse skin model and Strat-M membrane as an artificial skin model.

Results

A Carbopol-based MEH system of 20S-PPD was successfully prepared with a mean droplet size of 110 nm and narrow size distribution. The formulation was stable for 56 d, and its viscosity was high enough for its topical application. It significantly enhanced the in vitro and in vivo skin deposition of 20S-PPD with no influence on its systemic absorption in hairless mice. Notably, it was found that the Strat-M membrane provided skin deposition data well correlated to those obtained from the in vitro and in vivo mouse skin studies on 20S-PPD (correlation coefficient r 2 = 0.929‒0.947).

Conclusion

The MEH formulation developed in this study could serve as an effective topical delivery system for poorly soluble ginsenosides and their deglycosylated metabolites, including 20S-PPD.

SUBMITTER: Kim KT 

PROVIDER: S-EPMC6190503 | biostudies-literature | 2018 Oct

REPOSITORIES: biostudies-literature

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Microemulsion-based hydrogels for enhancing epidermal/dermal deposition of topically administered 20(<i>S</i>)-protopanaxadiol: <i>in vitro</i> and <i>in vivo</i> evaluation studies.

Kim Ki-Taek KT   Kim Min-Hwan MH   Park Ju-Hwan JH   Lee Jae-Young JY   Cho Hyun-Jong HJ   Yoon In-Soo IS   Kim Dae-Duk DD  

Journal of ginseng research 20170818 4


<h4>Background</h4>20(<i>S</i>)-Protopanaxadiol (20<i>S</i>-PPD) is a fully deglycosylated ginsenoside metabolite and has potent dermal antiaging activity. However, because of its low aqueous solubility and large molecular size, a suitable formulation strategy is required to improve its solubility and skin permeability, thereby enhancing its skin deposition. Thus, we optimized microemulsion (ME)-based hydrogel (MEH) formulations for the topical delivery of 20<i>S</i>-PPD.<h4>Methods</h4>MEs and  ...[more]

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