Solid lipid nanoparticle as an effective drug delivery system of a novel curcumin derivative: formulation, release in vitro and pharmacokinetics in vivo
CONTEXT: Curcumin (Cur) has a short duration of action which limits its therapeutic efficacy. Carbonic acid 17-(1,5-dimethyl-hexyl)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl ester 4-[7-(4-hydroxy-3-methoxy-phenyl)-3,5-dioxo-hepta-1,6-dienyl]-2...
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ftpubmed:oai:pubmedcentral.nih.gov:9704087 2023-05-15T15:52:49+02:00 Solid lipid nanoparticle as an effective drug delivery system of a novel curcumin derivative: formulation, release in vitro and pharmacokinetics in vivo Zhao, Wenmei Zeng, Mingtang Li, Ke Pi, Chao Liu, Zerong Zhan, Chenglin Yuan, Jiyuan Su, Zhilian Wei, Yuxun Wen, Jie Pi, Fengjuan Song, Xinjie Lee, Robert J. Wei, Yumeng Zhao, Ling 2022-11-23 http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9704087/ https://doi.org/10.1080/13880209.2022.2136205 en eng Taylor & Francis http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9704087/ http://dx.doi.org/10.1080/13880209.2022.2136205 © 2022 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. CC-BY Pharm Biol Research Article Text 2022 ftpubmed https://doi.org/10.1080/13880209.2022.2136205 2022-12-04T02:01:54Z CONTEXT: Curcumin (Cur) has a short duration of action which limits its therapeutic efficacy. Carbonic acid 17-(1,5-dimethyl-hexyl)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl ester 4-[7-(4-hydroxy-3-methoxy-phenyl)-3,5-dioxo-hepta-1,6-dienyl]-2-methoxy-phenyl ester (CUD), as a small molecule derivative of Cur with superior stability, has been developed in our laboratory. OBJECTIVE: CUD-loaded solid lipid nanoparticles (CUD-SLN) were prepared to prolong the duration of the drug action of Cur. MATERIALS AND METHODS: CUD-SLN were prepared with Poloxamer 188 (F68) and hydrogenated soybean phospholipids (HSPC) as carriers, and the prescription was optimized. The in vitro release of CUD and CUD-SLN was investigated. CUD-SLN (5 mg/kg) was injected into Sprague Dawley (SD) rats to investigate its pharmacokinetic behaviour. RESULTS: CUD-SLN features high entrapment efficiency (96.8 ± 0.4%), uniform particle size (113.0 ± 0.8 nm), polydispersity index (PDI) (0.177 ± 0.007) and an appropriate drug loading capacity (6.2 ± 0.1%). Optimized CUD-SLN exhibited sustained release of CUD for about 48 h. Moreover, the results of the pharmacokinetic studies showed that, compared to Cur, CUD-SLN had a considerably prolonged half-life of 14.7 h, slowed its metabolism in vivo by 35.6-fold, and had an improved area under the curve (AUC(0–)(t)) of 37.0-fold. CONCLUSIONS: CUD-SLN is a promising preparation for the development of a small molecule derivative of Cur. Text Carbonic acid PubMed Central (PMC) Pharmaceutical Biology 60 1 2300 2307 |
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Research Article |
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Research Article Zhao, Wenmei Zeng, Mingtang Li, Ke Pi, Chao Liu, Zerong Zhan, Chenglin Yuan, Jiyuan Su, Zhilian Wei, Yuxun Wen, Jie Pi, Fengjuan Song, Xinjie Lee, Robert J. Wei, Yumeng Zhao, Ling Solid lipid nanoparticle as an effective drug delivery system of a novel curcumin derivative: formulation, release in vitro and pharmacokinetics in vivo |
topic_facet |
Research Article |
description |
CONTEXT: Curcumin (Cur) has a short duration of action which limits its therapeutic efficacy. Carbonic acid 17-(1,5-dimethyl-hexyl)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl ester 4-[7-(4-hydroxy-3-methoxy-phenyl)-3,5-dioxo-hepta-1,6-dienyl]-2-methoxy-phenyl ester (CUD), as a small molecule derivative of Cur with superior stability, has been developed in our laboratory. OBJECTIVE: CUD-loaded solid lipid nanoparticles (CUD-SLN) were prepared to prolong the duration of the drug action of Cur. MATERIALS AND METHODS: CUD-SLN were prepared with Poloxamer 188 (F68) and hydrogenated soybean phospholipids (HSPC) as carriers, and the prescription was optimized. The in vitro release of CUD and CUD-SLN was investigated. CUD-SLN (5 mg/kg) was injected into Sprague Dawley (SD) rats to investigate its pharmacokinetic behaviour. RESULTS: CUD-SLN features high entrapment efficiency (96.8 ± 0.4%), uniform particle size (113.0 ± 0.8 nm), polydispersity index (PDI) (0.177 ± 0.007) and an appropriate drug loading capacity (6.2 ± 0.1%). Optimized CUD-SLN exhibited sustained release of CUD for about 48 h. Moreover, the results of the pharmacokinetic studies showed that, compared to Cur, CUD-SLN had a considerably prolonged half-life of 14.7 h, slowed its metabolism in vivo by 35.6-fold, and had an improved area under the curve (AUC(0–)(t)) of 37.0-fold. CONCLUSIONS: CUD-SLN is a promising preparation for the development of a small molecule derivative of Cur. |
format |
Text |
author |
Zhao, Wenmei Zeng, Mingtang Li, Ke Pi, Chao Liu, Zerong Zhan, Chenglin Yuan, Jiyuan Su, Zhilian Wei, Yuxun Wen, Jie Pi, Fengjuan Song, Xinjie Lee, Robert J. Wei, Yumeng Zhao, Ling |
author_facet |
Zhao, Wenmei Zeng, Mingtang Li, Ke Pi, Chao Liu, Zerong Zhan, Chenglin Yuan, Jiyuan Su, Zhilian Wei, Yuxun Wen, Jie Pi, Fengjuan Song, Xinjie Lee, Robert J. Wei, Yumeng Zhao, Ling |
author_sort |
Zhao, Wenmei |
title |
Solid lipid nanoparticle as an effective drug delivery system of a novel curcumin derivative: formulation, release in vitro and pharmacokinetics in vivo |
title_short |
Solid lipid nanoparticle as an effective drug delivery system of a novel curcumin derivative: formulation, release in vitro and pharmacokinetics in vivo |
title_full |
Solid lipid nanoparticle as an effective drug delivery system of a novel curcumin derivative: formulation, release in vitro and pharmacokinetics in vivo |
title_fullStr |
Solid lipid nanoparticle as an effective drug delivery system of a novel curcumin derivative: formulation, release in vitro and pharmacokinetics in vivo |
title_full_unstemmed |
Solid lipid nanoparticle as an effective drug delivery system of a novel curcumin derivative: formulation, release in vitro and pharmacokinetics in vivo |
title_sort |
solid lipid nanoparticle as an effective drug delivery system of a novel curcumin derivative: formulation, release in vitro and pharmacokinetics in vivo |
publisher |
Taylor & Francis |
publishDate |
2022 |
url |
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9704087/ https://doi.org/10.1080/13880209.2022.2136205 |
genre |
Carbonic acid |
genre_facet |
Carbonic acid |
op_source |
Pharm Biol |
op_relation |
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9704087/ http://dx.doi.org/10.1080/13880209.2022.2136205 |
op_rights |
© 2022 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
op_rightsnorm |
CC-BY |
op_doi |
https://doi.org/10.1080/13880209.2022.2136205 |
container_title |
Pharmaceutical Biology |
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60 |
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1 |
container_start_page |
2300 |
op_container_end_page |
2307 |
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1766387924606124032 |