Abstract
BackgroundCarrageenan (CRN), a polygalactan consisting of 15 to 40% ester sulfate, is used in oral controlled-release technology due to its viscosity and large molecular weight. Curcumin (Cur) is a highly potent antioxidant and anti-inflammatory agent against various diseases, such as tumors, liver disease, rheumatism, and Alzheimer’s disease. Although Cur shows excellent effects in the body, it has major problems, such as poor solubility and low bioavailability in water.MethodNanocomposites containing Cur were developed by emulsion technique. Cur@CRN was characterized through the viscosity measurement, size analysis, stability test, and loading efficiency. Antioxidant effects was analyzed with DPPH reagent, and anti-inflammatory effects was analyzed by NFkB/IkBr signaling pathway with wester blot. Cellular interaction was confirmed by flow cytometry and confocal images. Especially, permeability test was demonstrated in MDCK and Caco-2 monolayer cells.ResultsCur@CRN enhanced stability, antioxidant, and anti-inflammatory effects in vitro, compared with other polymer nanocomposites. Sulfate groups (SO42−) in CRN are transported across cell membranes by anion exchangers of the SLC26 gene families. We confirmed Caco-2 cells expressed SLC26A2 receptors interacted with CRN, expect for Tween 80 and hydroxypropyl cellulose. In contrary, other cells did not interact with CRN due to non-expression of SLC26A2 receptors. Based on this, Cur@CRN showed 44-fold better permeability than free Cur in MDCK cell assay.ConclusionEnhanced intestinal permeability of Cur can be applied in various health care facilities with significant antioxidant and anti-inflammatory effects compared with nonformulated Cur. Since the CRN composed of nanocomposites has a high molecular weight, high viscosity, and sulfate groups, it will be a platform that can increase the bioavailability of various insoluble drugs as well as Cur.
Highlights
Carrageenan (CRN), a polygalactan consisting of 15 to 40% ester sulfate, is used in oral controlledrelease technology due to its viscosity and large molecular weight
Sulfate groups (SO42−) in CRN are transported across cell membranes by anion exchangers of the solute carrier 26 (SLC26) gene families
Since the CRN composed of nanocomposites has a high molecular weight, high viscosity, and sulfate groups, it will be a platform that can increase the bioavailability of various insoluble drugs as well as Cur
Summary
Carrageenan (CRN), a polygalactan consisting of 15 to 40% ester sulfate, is used in oral controlledrelease technology due to its viscosity and large molecular weight. Carrageenan (CRN), a family of high-molecular-weight sulfated polysaccharides, is obtained from red seaweeds by extraction [1]. Administered drugs are absorbed systemically from the small intestine by influencing two major superfamilies of membrane transporters (ATP-binding cassette and solute carrier) [8, 9]. Sulfate transporters and anti-sigma factor antagonist domains have important roles in controlling the activity of sulfate transporters [20, 21] According to these properties, CRN with sulfate groups is recognized by SLC26A2; it can be well absorbed in the small intestine. The keto-form of Cur is able to convert to the enol-form to stabilize itself
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