Preparation, characterization, and ex vivo evaluation of isoxanthohumol nanosuspension.

Autor: Zhang M; School of Pharmacy Heilongjiang University of Chinese Medicine, Key Laboratory of Basic and Application Research of Beiyao (Heilongjiang University of Chinese Medicine), Ministry of Education 150040, China., Liu T; School of Pharmacy Heilongjiang University of Chinese Medicine, Key Laboratory of Basic and Application Research of Beiyao (Heilongjiang University of Chinese Medicine), Ministry of Education 150040, China., Tan D; School of Pharmacy Fuzhou University, China., Liu J; School of Pharmacy Heilongjiang University of Chinese Medicine, Key Laboratory of Basic and Application Research of Beiyao (Heilongjiang University of Chinese Medicine), Ministry of Education 150040, China., Gao Y; School of Pharmacy Heilongjiang University of Chinese Medicine, Key Laboratory of Basic and Application Research of Beiyao (Heilongjiang University of Chinese Medicine), Ministry of Education 150040, China., Wang H; School of Pharmacy Heilongjiang University of Chinese Medicine, Key Laboratory of Basic and Application Research of Beiyao (Heilongjiang University of Chinese Medicine), Ministry of Education 150040, China., Gao F; School of Pharmacy Heilongjiang University of Chinese Medicine, Key Laboratory of Basic and Application Research of Beiyao (Heilongjiang University of Chinese Medicine), Ministry of Education 150040, China., Yang Z; School of Pharmacy Heilongjiang University of Chinese Medicine, Key Laboratory of Basic and Application Research of Beiyao (Heilongjiang University of Chinese Medicine), Ministry of Education 150040, China. Electronic address: zhixin.y@163.com.
Jazyk: angličtina
Zdroj: International journal of pharmaceutics [Int J Pharm] 2024 Dec 25; Vol. 667 (Pt B), pp. 124909. Date of Electronic Publication: 2024 Nov 08.
DOI: 10.1016/j.ijpharm.2024.124909
Abstrakt: This study assessed the equilibrium solubility, oil-water distribution coefficient, and dissociation constant of Isoxanthohumol (IXN), and formulated IXN nanoparticles (IXN-Nps) using a micro media grinding method. The research characterized the particle size, polydispersity index, zeta potential, morphology, and structure of the nanoparticles, and evaluated the optimal cryoprotectant. Additionally, the study examined the toxicity and in vitro and in vivo release of IXN on HT-29 cells. IXN is classified as a Biopharmaceutical Classification System (BCS) II class drug with weak acidity. The average particle size of IXN-Nps is 249.500 nm, with a polydispersity index (PDI) of 0.149 and a zeta potential of -25.210 mV. The research identified 5 % mannitol as the optimal cryoprotectant. Compared to IXN, the half-maximal inhibitory concentration of IXN-Nps decreased to one-third, demonstrating a significant inhibitory effect on HT-29 colon cancer cells. The in vitro cumulative release rate of IXN-Nps within 24 h was 3.5 times higher than that of the IXN solution. In vivo pharmacokinetic results revealed that the oral bioavailability of IXN-Nps increased significantly by 2.8 times compared to the IXN solution. The correlation coefficient (r = 0.9227) exceeded the critical value for significance at the 0.01 (r = 0.834) level, indicating a strong correlation between in vivo and in vitro results. Consequently, the nanosuspension overcame the low solubility limitation of IXN and proved to be an effective method for enhancing the oral bioavailability of IXN.
Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2024 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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