Abstract
Oral delivery is considered the preferred route of administration due to its convenience and favorable compliance. However, this delivery often faces difficulties, such as poor solubility, limited absorption, and undesirable stability, especially for some volatile oils. The aim of this study was to develop self-emulsifying drug delivery systems (SEDDS) containing cinnamaldehyde (CA) to overcome these shortcomings. The CA-SEDDS were spherical and smooth with an average size of 14.96 ± 0.18 nm. Differential scanning calorimetry (DSC) and attenuated total reflection by Fourier transform infrared (ATR-FTIR) showed that CA has been successfully loaded into SEDDS. The accumulative release of CA-SEDDS (73.39%) was approximately 2.14-fold that of free CA when using simulated intestinal fluid as the release medium. A scanning electron microscope was used to observe the mucus network structure. Rheological tests found that CA-SEDDS can appropriately enhance the viscosity of the mucus system. We found from tissue distribution studies that CA was more widely distributed in various tissues in the CA-SEDDS group compared to the free CA group. The cinnamaldehyde and cinnamon acid also accumulated more in various tissues in the CA-SEDDS group than in the free CA group, especially in the kidney. These findings hinted that SEDDS exhibited lower irritation, good release, and penetration, which demonstrated great potential for utilizing CA. Our research supports the rational implications of SEDDS in delivering similar volatile substances by improving the solubility, mucus penetration, and stability, resulting in excellent clinical efficacy.
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Data Availability
The datasets used or analyzed during the current study are available from the corresponding author on reasonable request.
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The authors gratefully acknowledge support from the National Natural Science Foundation of China (No. 81803831), Key University Natural Science Research Project of Anhui Province (KJ2018A0301).
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Wenxuan Cao: Contributed significantly to editing the manuscript in major revisions. Mengqiu Xia: investigation, writing—review and editing. Chunling Tian: Software, Data curation. Wenqing Wu: writing—review and editing. Ye Cai: writing—review and editing. Xiaoqin Chu: conceptualization, funding acquisition, project administration, writing—review and editing, supervision.
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Liu, L., Cao, W., Xia, M. et al. Self-Emulsifying Drug Delivery System Enhances Tissue Distribution of Cinnamaldehyde by Altering the Properties of the Mucus Layer. AAPS PharmSciTech 23, 261 (2022). https://doi.org/10.1208/s12249-022-02416-4
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DOI: https://doi.org/10.1208/s12249-022-02416-4