1. Solid lipid nanoparticle as an effective drug delivery system of a novel curcumin derivative: formulation, release in vitro and pharmacokinetics in vivo.
- Author
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Wenmei Zhao, Mingtang Zeng, Ke Li, Chao Pi, Zerong Liu, Chenglin Zhan, Jiyuan Yuan, Zhilian Su, Yuxun Wei, Jie Wen, Fengjuan Pi, Xinjie Song, Lee, Robert J., Yumeng Wei, and Ling Zhao
- Subjects
DRUG delivery systems ,NANOPARTICLES ,SMALL molecules ,CURCUMIN ,NANOMEDICINE ,PHARMACOKINETICS - Abstract
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 (5mg/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 ± 0.8nm), 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 (AUC0-t) of 37.0-fold. Conclusions: CUD-SLN is a promising preparation for the development of a small molecule derivative of Cur. [ABSTRACT FROM AUTHOR]
- Published
- 2022
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