In vitro and in vivo evaluation of cinnamaldehyde Microemulsion–Mucus interaction

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Abstract

The current investigation explores the possible mechanism of the microemulsion drug delivery system to improve the oral bioavailability of cinnamaldehyde (CA), an important food spice, from the perspective of the microemulsion-mucus system. The cinnamaldehyde microemulsion (CA-ME) was prepared by the water titration method combined with the pseudo-ternary phase diagram. The dynamic analysis was applied to detect the drug release in vitro. An intestinal mucosal injury test was conducted to evaluate the safety of CA-ME and drug absorption across the intestinal tract of rats was investigated through an Ussing chamber system. The rheology of blank mucus and drug-loaded mucus was investigated using a rheometer. The bioavailability of CA-ME in rats was evaluated through pharmacokinetic characteristics. The ratio of optimal prescription was Tween 80: 1,2-propanediol: vitamin E oil: CA: water = 24.3:4.8:5:7.5:58.4. The droplets were uniform in size and evenly dispersed. Rheological studies showed that the microemulsion-mucus system all exhibit pseudoplastic fluid behavior, and CA-ME increased the viscosity of the mucus to a certain extent. Compared with CA solution, CA-ME promoted the absorption of CA in various intestinal segments, especially the ileum. Pharmacokinetic experiments showed that the relative bioavailability of CA-ME was enhanced 2.5-fold higher than that of CA solution. ME as a carrier for lipophobic substances, may increase the viscosity of the intestine mucus system to obtain longer residue time and better absorption. PRACTICAL APPLICATIONS: In this study, in vitro absorption Ussing model was combined with rheological and pharmacokinetic analysis to systematically analyze the intestinal mucus mechanism of microemulsion to improve the oral bioavailability of cinnamic aldehyde. It laid the foundation for exploring the absorption and transport of drugs in the intestinal mucus barrier.

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