Solid lipid nanoparticle as an effective drug delivery system of a novel curcumin derivative: formulation, release in vitro and pharmacokinetics in vivo. (31st December 2022)

• Record Type: Journal Article
• Authors: 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
• Is Part Of: Pharmaceutical biology. Volume 60:Number 1(2022)
• Page Start: 2300
• Page End: 2307
• Publication Date: 2022-12-31
• Subjects: Small molecule derivative of curcumin -- Poloxamer 188 -- nanotechnology; Pharmacognosy -- Periodicals; Materia medica, Vegetable -- Periodicals; 615.321
• DOI: 10.1080/13880209.2022.2136205
• Languages: English
• ISSNs: 1388-0209

Abstract

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 (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 (AUC0– t ) of 37.0-fold. Conclusions: CUD-SLN is a promising preparation for the development of a small molecule derivative of Cur.