Sheng Chang
The Increased Dissolution and Oral Absorption of Itraconazole by Nanocrystals with an Endogenous Small-Molecule Surfactant as a Stabilizer
Chang, Sheng; Yang, Qiang; Liu, Jiahuan; Yin, Li; Han, Jihong; Zong, Lanlan; Pu, Xiaohui
Abstract
The aim of this study was to develop cholic-acid-stabilized itraconazole nanosuspensions (ITZ-Nanos) with the objective of enhancing drug dissolution and oral absorption. A laboratory-scale microprecipitation–high-pressure homogenization method was employed for the preparation of the ITZ-Nanos, while dynamic light scattering, transmission electron microscope analysis, X-ray diffraction, differential scanning calorimetry, and high-performance liquid chromatography analysis were utilized to evaluate their physicochemical properties. The absorption and bioavailability of the ITZ-Nanos were assessed using Caco-2 cells and rats, with Sporanox® pellets as a comparison. Prior to lyophilization, the particle size of the ITZ-Nanos measured approximately 225.7 nm. Both X-ray diffraction and differential scanning calorimetry confirmed that the ITZ remained crystalline within the nanocrystals. Compared to the pellets, the ITZ-Nanos exhibited significantly higher levels of supersaturation dissolution and demonstrated enhanced drug uptake by the Caco-2 cells. The AUC(0–t) value for the ITZ-Nanos in rats was 1.33-fold higher than that observed for the pellets. These findings suggest that cholic acid holds promise as a stabilizer for ITZ nanocrystals, as well as potentially other nanocrystals.
Citation
Chang, S., Yang, Q., Liu, J., Yin, L., Han, J., Zong, L., & Pu, X. (in press). The Increased Dissolution and Oral Absorption of Itraconazole by Nanocrystals with an Endogenous Small-Molecule Surfactant as a Stabilizer. Molecules, 29(8), Article 1769. https://doi.org/10.3390/molecules29081769
Journal Article Type | Article |
---|---|
Acceptance Date | Apr 10, 2024 |
Online Publication Date | Apr 13, 2024 |
Deposit Date | Apr 29, 2024 |
Journal | Molecules |
Electronic ISSN | 1420-3049 |
Publisher | MDPI |
Peer Reviewed | Peer Reviewed |
Volume | 29 |
Issue | 8 |
Article Number | 1769 |
DOI | https://doi.org/10.3390/molecules29081769 |
Keywords | itraconazole; nanocrystals; cholic acid; supersaturation dissolution; in vivo pharmacokinetics; bioavailability |
Public URL | https://keele-repository.worktribe.com/output/799779 |
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