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Updated: Jan 11, 2026

Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
Spray-Dried Inclusion Complex of Apixaban with β-Cyclodextrin Derivatives: Characterization, Solubility, and
Da Young Song1, Jeong Gyun Lee1, Kyeong Soo Kim1
1Department of Pharmaceutical Engineering, Gyeongsang National University, 33 Dongjin-ro, Jinju 52725, Republic of Korea.
None:
Apixaban (APX) is a direct oral anticoagulant with low aqueous solubility and limited bioavailability. This study aimed to improve APX solubility by forming spray-dried inclusion complexes (ICs) with β-cyclodextrin (β-CD) derivatives. ICs were prepared using hydroxypropyl-β-CD (HP-β-CD), sulfobutylether-β-CD (SBE-β-CD), randomly methylated-β-CD (RM-β-CD), and heptakis(2,6-di-O-methyl)-β-CD (DM-β-CD). Complex formation (1:1 stoichiometry) was confirmed by phase solubility studies and Job's plots. The ICs were characterized by SEM, PXRD, DSC, and FTIR, and their saturated solubility was evaluated. Molecular docking assessed host-guest interactions. Among the tested carriers, DM-β-CD exhibited the highest stability constant (KC = 371.92 M-1) and produced amorphous ICs. DM-ICs achieved the greatest solubility enhancement at all pH conditions, with a maximum solubility of 1968.7 μg/mL at pH 1.2 and ~78.7-fold increase in water compared with pure APX. Docking results supported stable inclusion with the lowest binding free energy (-8.01 kcal/mol). These findings indicate that DM-β-CD-based ICs effectively enhance APX dissolution and show potential as solubilizing carriers for oral dosage forms.
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