Abstract
Curcumin (CUR), a polyphenolic substance extracted from plants, has extensive pharmacological activities. However, CUR is difficult to be absorbed in the body due to its poor stability and low solubility. Studies have found that cochleates can be used as a new delivery system to encapsulate bioactive agents for the purpose of improving its stability and bioavailability. In this study, thin-film dispersion and trapping methods were used to prepare curcumin-loaded cochleates (CUR-Cochs). Then CUR-Cochs were characterized and the encapsulation efficiency was determined by HPLC. In addition, the freeze-drying process of CUR-Cochs was studied and related characterization was performed. CCK-8 assay was used to detect the cytotoxicity of cochleates carrier. Additionally, H2O2-induced cellular oxidative damage model were used to evaluate its antioxidant capacity. The results showed that the structure of CUR-Cochs was a spiral cylinder with an average particle size of 463.8 nm and zeta potential of −15.47 mV. The encapsulation efficiency was the highest (83.66 ± 0.8)% with 1:50 CUR-to-lipid mass ratio. In vitro results showed that cochleates had negligible cytotoxicity and owned antioxidant capacity, which provided the possibility for their applications in food and medicine. In general, the method herein might be a promising method to encapsulate CUR for further use as a bioactive agent in functional foods.
Highlights
IntroductionIt is a natural active substance that is insoluble in water and soluble in organic solvents such as ethanol, methanol, and glacial acetic acid [3]
Low solubility, poor stability and low bioavailability have been the bottleneck for further development and utilization of CUR
10–100 μL CaCl2 was added to the CUR-Lipos solution respectively with constant low-speed stirring at 60 ◦ C to observe the formation process of cochleates
Summary
It is a natural active substance that is insoluble in water and soluble in organic solvents such as ethanol, methanol, and glacial acetic acid [3]. CUR has a good clinical safety profile, and clinical trials found that CUR was well tolerated even when administered orally at a dose of 12 g per day for 3 months [8]. Shortcomings of CUR—such as poor water solubility, poor chemical stability, high metabolic rate, and low bioavailability—have become obstacles for its further applications [9–11]. The bioavailability study of CUR is very important. The bioavailability of CUR is poor due to their low solubility in water and stability issues [12]. Due to the hydrophobicity of CUR, only a small amount of oral CUR is absorbed by the small intestine and reaches the systemic circulation [13,14]. The absorbed CUR is rapidly metabolized by the liver in the body, and excreted through the renal system, further deteriorating its
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