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CC BY-NC-ND 4.0 · Journal of Health and Allied Sciences NU 2022; 12(03): 312-321
DOI: 10.1055/s-0041-1741417
Original Article

Composition of Piperine with Enteric-Coated Chitosan Microspheres Enhances the Transepithelial Permeation of Curcumin in Sheep Intestinal Mucosa and Caco-2 Cells

Githa Thomas
1   Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, Nitte (Deemed to be University), Mangalore, Karnataka, India
,
Marina Koland 
1   Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, Nitte (Deemed to be University), Mangalore, Karnataka, India
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Abstract

Objectives The purpose of this study was to investigate the efficacy of enteric-coated chitosan microspheres with herbal bioenhancer, piperine, as a suitable composition for improving the permeation of curcumin through biological membranes using suitable ex vivo models.

Material and Methods Chitosan microspheres of curcumin and piperine were prepared by an emulsion cross-linking method using glutaraldehydes the cross-linking agent and characterized for size, shape, entrapment efficiency, mucoadhesion, and in vitro release. The effect of piperine on the permeation of curcumin through excised sheep intestinal mucosa and Caco-2-cell monolayer was investigated.

Statistical Analysis The data from permeation studies were analyzed by Student's t-test using Statistical Package for the Social Sciences (SPSS) software (SPSS, Chicago, IL, United States) with p-values <0.05 indicating statistical significance.

Results The formulations showed mucoadhesion for a period of more than 6 hours which was influenced by the chitosan content. The rate of drug release of uncoated formulation followed first-order kinetics, and the mechanism of release was non-Fickian transport. Optimized formulation was coated with a pH-sensitive polymer, Eudragit S-100, by a solvent evaporation technique in different concentrations and evaluated for ex vivo permeation through sheep intestinal mucosa and Caco-2-cell monolayer. Scanning electron microscopy images of the optimized coated formulation showed spherical particles with smooth surfaces. The calculated permeation flux and permeability coefficient of curcumin from microspheres were at least 20% greater in the presence of piperine through the intestinal mucosa and 30% through the Caco-2-cell monolayer model. The permeability coefficient of curcumin from microspheres with piperine was 1.93 × 10 to 5 cm/sec and significantly greater (p < 0.05) than that of microspheres devoid of piperine and from aqueous dispersion (p < 0.005).

Conclusion The study confirmed the contribution of piperine and mucoadhesive microspheres toward improved permeation of curcumin through biological membranes, thereby providing an approach that has the potential of increasing transport through intestinal epithelial cells and possibly enhancing the oral bioavailability of this drug.

Keywords

bioenhancer - curcumin - chitosan - enteric coating - microspheres - piperine


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Artikel online veröffentlicht:
18. Januar 2022

© 2022. Nitte (Deemed to be University). This is an open access article published by Thieme under the terms of the Creative Commons Attribution-NonDerivative-NonCommercial License, permitting copying and reproduction so long as the original work is given appropriate credit. Contents may not be used for commercial purposes, or adapted, remixed, transformed or built upon. (https://creativecommons.org/licenses/by-nc-nd/4.0/)

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