Abstract
This study aimed to investigate the influence of the microemulsion with essential oil from Zanthoxylum bungeanum Maxim. as oil phase (ZO-ME) on skin permeation of drugs with different lipophilicity (logP values ranging from −1.01 to 3.85) and explain its underlying mechanism. A series of components with different logP values were selected as model drugs and their transdermal behaviors were examined using Franz diffusion cell method. Furthermore, the influence of ZO-ME on keratin, intercellular lipids and microstructure of the stratum corneum (SC) was evaluated by attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC) studies and hematoxylin-eosin (HE) staining. The transdermal translocation of ZO-ME was visualized by confocal laser scanning microscope (CLSM). In vitro skin permeation studies showed that ZO-ME had a good permeation enhancement effect on drugs with different lipophilicity, especially for drugs with a logP value of −0.5. The permeation enhancement effect of ZO-ME may depend on affecting the order of the SC lipids, changing lipid fluidity and protein conformation, destroying the integrity of the SC structure. Moreover, the observation by CLSM showed that ZO-ME could partially penetrate through the SC and reach the dermis in its intact form. Futhermore, the oil phase of ZO-ME, Z. bungeanum oil, played an important role in its permeation enhancement effect and permeation form (intact or not). As the combination of Z. bungeanum oil and microemulsion, ZO-ME could not only increase the permeation enhancement effect of microemulsion, but also reduce the irritation of Z. bungeanum oil.
Published Version
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