Improving the Dissolution Rate and Bioavailability of Curcumin via Co-Crystallization

Abstract

Curcumin (CUR) is a natural polyphenolic compound with various pharmacological activities. Low water solubility and bioavailability limit its clinical application. In this work, to improve the bioavailability of CUR, we prepared a new co-crystal of curcumin and L-carnitine (CUR-L-CN) via liquid-assisted grinding. Both CUR and L-CN have high safe dosages and have a wide range of applications in liver protection and animal nutrition. The co-crystal was fully characterized and the crystal structure was disclosed. Dissolution experiments were conducted in simulated gastric fluids (SGF) and simulated intestinal fluids (SIF). CUR-L-CN exhibited significantly faster dissolution rates than those of pure CUR. Hirshfeld surface analysis and wettability testing indicate that CUR-L-CN has a higher affinity for water and thus exhibits faster dissolution rates. Pharmacokinetic studies were performed in rats and the results showed that compared to pure CUR, CUR-L-CN exhibited 6.3-times-higher AUC0–t and 10.7-times-higher Cmax.

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“…Possible explanations are as follows: the catechol groups of CUR, and the primary amino groups of PDA can interact through hydrogen bonding [36], and the interaction force between CUR and PDA reaches the maximum or saturation when the CUR concentration is 1.5 mg/mL. As the concentration of CUR continues to increase, the repulsive force increases, hydrogen bonds weaken, and the loading decreases [37].…”

“…The deconvoluted peaks at ca. 400.0 eV, 401.6 eV, and 402.8 eV can be observed in the spectrum of N 1s (Figure 4c), which are attributed to -NH=, -NH-, and -N + H-, respectively, where the -NH-bond serves as the connection between PDA and CUR [37]. Additionally, C=O and C-O bonds can be detected at 531.3 eV and 533.1 eV in the spectrum of O 1s (Figure 4d).…”