SEDDS facilitate cinnamaldehyde crossing the mucus barrier: The perspective of mucus and Caco-2/HT29 co-culture models

[Display omitted] Self-emulsifying drug delivery systems (SEDDS) have potential applications in the delivery of hydrophobic components. Oral drugs are readily captured and cleared by intestinal mucus, a natural barrier that covers the mucosal epithelium and prevents the entry of foreign substances....

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Bibliographic Details
Published in:International journal of pharmaceutics 2022-02, Vol.614, p.121461-121461, Article 121461
Main Authors: Cai, Ye, Liu, Liu, Xia, Mengqiu, Tian, Chunling, Wu, Wenqing, Dong, Baoqi, Chu, Xiaoqin
Format: Article
Language:English
Subjects:
Acrolein - analogs & derivatives
Animals
Caco-2 cell
Caco-2 Cells
Cinnamaldehyde
Coculture Techniques
Drug Delivery Systems
Emulsions
HT29 cell
Humans
Mucus
Pharmacokinetics
Rats
SEDDS
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Summary:[Display omitted] Self-emulsifying drug delivery systems (SEDDS) have potential applications in the delivery of hydrophobic components. Oral drugs are readily captured and cleared by intestinal mucus, a natural barrier that covers the mucosal epithelium and prevents the entry of foreign substances. In this study, we investigated for the first time the ability of SEDDS to deliver the lipophilic aldehyde cinnamaldehyde (CA-SEDDS) in rat mucus, mucin solution, Caco-2 and Caco-2/HT29 co-culture monolayer systems. CA-SEDDS was characterized by particle size, Zeta potential and the logDSEDDS/release medium. The capacity of CA-SEDDS to enhance mucus permeability was investigated in rat intestinal mucus gel and mucin solution with the period of in 12 h by Transwell® diffusion. We evaluated the potential of CA-SEDDS delivery of CA in a co-culture system of absorptive Caco-2 and mucus-secreting HT29 cells. CA-SEDDS exhibited excellent mucus permeability in mucus and mucin solutions, 5.1- and 2.8-fold higher than the free CA group, respectively. CA-SEDDS penetration increased by 2.5-fold compared with free CA when using the mucus-secreting co-culture cell model as a barrier. The relative oral bioavailability of CA-SEDDS was 242% compared to CA without formulation. These findings suggest that SEDDS exhibited good release and superior mucus permeability, displaying great potential for the future of hydrophobic oral applications.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2022.121461