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Lipid/Clay-Based Solid Dispersion Formulation for Improving the Oral Bioavailability of Curcumin

This study was conducted to develop a lipid/clay-based solid dispersion (LSD) formulation to enhance the dissolution and oral bioavailability of poorly soluble curcumin. Krill oil and aminoclay were used as a lipid and a stabilizer, respectively, and LSD formulations of curcumin were prepared by an...

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Autores principales: Song, Jae Geun, Noh, Hye-Mi, Lee, Sang Hoon, Han, Hyo-Kyung
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9697399/
https://www.ncbi.nlm.nih.gov/pubmed/36365088
http://dx.doi.org/10.3390/pharmaceutics14112269
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author Song, Jae Geun
Noh, Hye-Mi
Lee, Sang Hoon
Han, Hyo-Kyung
author_facet Song, Jae Geun
Noh, Hye-Mi
Lee, Sang Hoon
Han, Hyo-Kyung
author_sort Song, Jae Geun
collection PubMed
description This study was conducted to develop a lipid/clay-based solid dispersion (LSD) formulation to enhance the dissolution and oral bioavailability of poorly soluble curcumin. Krill oil and aminoclay were used as a lipid and a stabilizer, respectively, and LSD formulations of curcumin were prepared by an antisolvent precipitation method combined with freeze-drying process. Based on the dissolution profiles, the optimal composition of LSD was determined at the weight ratio of curcumin: krill oil: aminoclay of 1:5:5 in the presence of 0.5% of D-α-tocopherol polyethylene glycol succinate. The structural and morphological characteristics of the LSD formulation were determined using X-ray powder diffraction, differential scanning calorimetry, and scanning electron microscopy. Crystalline curcumin was changed to an amorphous form in the LSD formulation. At the pH of acidic to neutral, the LSD formulation showed almost complete drug dissolution (>90%) within 1 h, while pure curcumin exhibited minimal dissolution of less than 10%. Furthermore, the LSD formulation had significantly improved oral absorption of curcumin in rats, where C(max) and AUC of curcumin were 13- and 23-fold higher for the LSD formulation than for the pure drug. Taken together, these findings suggest that the krill oil-based solid dispersion formulation of curcumin effectively improves the dissolution and oral bioavailability of curcumin.
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spelling pubmed-96973992022-11-26 Lipid/Clay-Based Solid Dispersion Formulation for Improving the Oral Bioavailability of Curcumin Song, Jae Geun Noh, Hye-Mi Lee, Sang Hoon Han, Hyo-Kyung Pharmaceutics Article This study was conducted to develop a lipid/clay-based solid dispersion (LSD) formulation to enhance the dissolution and oral bioavailability of poorly soluble curcumin. Krill oil and aminoclay were used as a lipid and a stabilizer, respectively, and LSD formulations of curcumin were prepared by an antisolvent precipitation method combined with freeze-drying process. Based on the dissolution profiles, the optimal composition of LSD was determined at the weight ratio of curcumin: krill oil: aminoclay of 1:5:5 in the presence of 0.5% of D-α-tocopherol polyethylene glycol succinate. The structural and morphological characteristics of the LSD formulation were determined using X-ray powder diffraction, differential scanning calorimetry, and scanning electron microscopy. Crystalline curcumin was changed to an amorphous form in the LSD formulation. At the pH of acidic to neutral, the LSD formulation showed almost complete drug dissolution (>90%) within 1 h, while pure curcumin exhibited minimal dissolution of less than 10%. Furthermore, the LSD formulation had significantly improved oral absorption of curcumin in rats, where C(max) and AUC of curcumin were 13- and 23-fold higher for the LSD formulation than for the pure drug. Taken together, these findings suggest that the krill oil-based solid dispersion formulation of curcumin effectively improves the dissolution and oral bioavailability of curcumin. MDPI 2022-10-24 /pmc/articles/PMC9697399/ /pubmed/36365088 http://dx.doi.org/10.3390/pharmaceutics14112269 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Song, Jae Geun
Noh, Hye-Mi
Lee, Sang Hoon
Han, Hyo-Kyung
Lipid/Clay-Based Solid Dispersion Formulation for Improving the Oral Bioavailability of Curcumin
title Lipid/Clay-Based Solid Dispersion Formulation for Improving the Oral Bioavailability of Curcumin
title_full Lipid/Clay-Based Solid Dispersion Formulation for Improving the Oral Bioavailability of Curcumin
title_fullStr Lipid/Clay-Based Solid Dispersion Formulation for Improving the Oral Bioavailability of Curcumin
title_full_unstemmed Lipid/Clay-Based Solid Dispersion Formulation for Improving the Oral Bioavailability of Curcumin
title_short Lipid/Clay-Based Solid Dispersion Formulation for Improving the Oral Bioavailability of Curcumin
title_sort lipid/clay-based solid dispersion formulation for improving the oral bioavailability of curcumin
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9697399/
https://www.ncbi.nlm.nih.gov/pubmed/36365088
http://dx.doi.org/10.3390/pharmaceutics14112269
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