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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| Format: | Article |
| Language: | English |
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MDPI AG
2022-10-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/11/2269 |
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| author | Jae Geun Song Hye-Mi Noh Sang Hoon Lee Hyo-Kyung Han |
| author_facet | Jae Geun Song Hye-Mi Noh Sang Hoon Lee Hyo-Kyung Han |
| author_sort | Jae Geun Song |
| collection | DOAJ |
| 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<sub>max</sub> 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. |
| first_indexed | 2024-03-09T18:45:28Z |
| format | Article |
| id | doaj.art-d6865a89a3ce4dd18fb4eda6f6b980c1 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T18:45:28Z |
| publishDate | 2022-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-d6865a89a3ce4dd18fb4eda6f6b980c12023-11-24T06:19:23ZengMDPI AGPharmaceutics1999-49232022-10-011411226910.3390/pharmaceutics14112269Lipid/Clay-Based Solid Dispersion Formulation for Improving the Oral Bioavailability of CurcuminJae Geun Song0Hye-Mi Noh1Sang Hoon Lee2Hyo-Kyung Han3BK21 FOUR Team and Integrated Research Institute for Drug Development, College of Pharmacy, Dongguk University-Seoul, Dongguk-ro-32, Ilsan-Donggu, Goyang 10326, KoreaBK21 FOUR Team and Integrated Research Institute for Drug Development, College of Pharmacy, Dongguk University-Seoul, Dongguk-ro-32, Ilsan-Donggu, Goyang 10326, KoreaBK21 FOUR Team and Integrated Research Institute for Drug Development, College of Pharmacy, Dongguk University-Seoul, Dongguk-ro-32, Ilsan-Donggu, Goyang 10326, KoreaBK21 FOUR Team and Integrated Research Institute for Drug Development, College of Pharmacy, Dongguk University-Seoul, Dongguk-ro-32, Ilsan-Donggu, Goyang 10326, KoreaThis 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<sub>max</sub> 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.https://www.mdpi.com/1999-4923/14/11/2269curcuminkrill oillipid-based formulationaminoclayantisolvent precipitation |
| spellingShingle | Jae Geun Song Hye-Mi Noh Sang Hoon Lee Hyo-Kyung Han Lipid/Clay-Based Solid Dispersion Formulation for Improving the Oral Bioavailability of Curcumin Pharmaceutics curcumin krill oil lipid-based formulation aminoclay antisolvent precipitation |
| 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 | curcumin krill oil lipid-based formulation aminoclay antisolvent precipitation |
| url | https://www.mdpi.com/1999-4923/14/11/2269 |
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