ACS Omega· 2026Q1
Fast-Dissolving and Highly Soluble Dasatinib Multicomponent Crystals Efficiently Inhibit Leukemia Cell Viability
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- Q1SCImago
- 2026year
Short summary
New multicomponent crystalline forms (MCCs) of dasatinib (DAS) achieved up to 1470-fold higher aqueous solubility and 312-fold increased intrinsic dissolution rate compared to the parent drug, leading to enhanced cytotoxicity against tumor cells.
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Key points
- Two novel multicomponent crystalline forms (MCCs) of dasatinib were synthesized and characterized.
- MCCs exhibited up to 1470-fold enhancement in buffered aqueous solubility versus parent dasatinib.
- Intrinsic dissolution rate increased by up to 312-fold for the MCCs.
- Dasatinib MCCs showed increased cytotoxicity and selectivity toward tumor cells.
AI-generated from the title and abstract; the full text is not read.
Abstract
Abstract Dasatinib (DAS) is a biopharmaceutical classification system (BCS) class II drug that is used orally to treat chronic myelogenous leukemia. However, its very low and pH-dependent aqueous solubility severely limits its oral bioavailability. To address this biopharmaceutical limitation, we designed more soluble multicomponent crystalline forms (MCCs) of DAS. Two novel salt solvate forms were successfully obtained via solvent evaporation through reactions with maleic and fumaric acids. A comprehensive solid-state evaluation of these salt solvate forms was conducted by using X-ray diffraction (SCXRD, PXRD), spectroscopy (FT-IR and 1H NMR), and thermal (TG and DSC) analyses. Both MCCs of DAS have displayed substantial enhancements in buffered aqueous solubility (up 1470-fold) and intrinsic dissolution rate (up 312-fold) compared with the parent drug. Furthermore, the DAS MCCs exhibited an increased cytotoxicity and selectivity toward tumor cells. These fulfillments highlight the potential of crystalline salt engineering to enhance the unsatisfactory oral bioavailability and anticancer efficacy of the DAS.
The authors' abstract, as published at the source. ACS Omega, 2026 · DOI ↗
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Field: Hematology
HematologyMedicine