FORMULATING A β CYCLODEXTRIN–DASATINIB INCLUSION COMPLEX BY KNEADING TO BOOST DISSOLUTION PERFORMANCE

Authors

  • VANITHA SURESHKUMAR Department of Pharmacy Practice, Vinayaka Mission’s College of Pharmacy, Vinayaka Mission’s Research Foundation (Deemed to be University), Salem-636008, Tamil Nadu, India. Department of Pharmaceutics, The Erode College of Pharmacy, Erode-638112, Tamil Nadu, India https://orcid.org/0009-0004-8844-0568
  • KOTHAI RAMALINGAM Department of Pharmacy Practice, Vinayaka Mission’s College of Pharmacy, Vinayaka Mission’s Research Foundation (Deemed to be University), Salem-636008, Tamil Nadu, India https://orcid.org/0000-0002-4571-0917
  • ARUL BALASUBRAMANIAN Department of Pharmacy Practice, Vinayaka Mission’s College of Pharmacy, Vinayaka Mission’s Research Foundation (Deemed to be University), Salem-636008, Tamil Nadu, India https://orcid.org/0000-0001-6896-5069

DOI:

https://doi.org/10.22159/ijap.2026v18i4.58035

Keywords:

Dasatinib, β-Cyclodextrin, Inclusion complex, Kneading method, Phase solubility, Dissolution enhancement

Abstract

Objective: Dasatinib (DAS) is a class II BCS tyrosine kinase inhibitor whose clinical efficacy is hindered by limited aqueous solubility. “A simple β-cyclodextrin (β-CD) inclusion complex was formulated to improve its pre-absorptive performance.” Ingredients were DAS and β-CD (97%); the complex was formulated at the optimum molar ratio of 2:1(β-CD: DAS)

Methods: Dasatinib –β-cyclodextrin (β-CD: DAS) inclusion complex was prepared by using kneading method and evaluated for the phase solubility studies, stoichiometric ratio, saturation solubility, drug content and in-vitro drug release profiles. The inclusion complex was characterized by using FTIR, XRD, DSC &1H NMR studies.

Results: The complex enhanced aqueous solubility from ~14 µg/mL (neat DAS) to ~40.15 µg/mL (~3-fold). Phase-solubility profiling indicated an AL-type response; combined with a Job's plot maximum at R ≈ 0.7, evidence favored a suitable 2:1 β-CD: DAS stoichiometry with moderate affinity consistent with fast release. In USP-II dissolution (pH 6.8, 37 °C), the complex delivered ~76.90% drug release at 120 min compared to ~35.9% for DAS. 

Conclusion: FTIR band overlap/attenuation (N–H, C=O, C–O–C/ O–H), loss of the DAS melting endotherm on DSC, reduced/broadened XRD reflections, and SEM-documented loss of crystalline habit, along with ^1H NMR chemical-shift perturbations (β-CD H-3/H-5; DAS protons), confirmed true inclusion in place of physical admixture. Overall, kneaded β-CD complexation forms a strong, cost-effective pathway to convert DAS into a dispersion and dissolution-capable product with evident promise to enhance oral availability.

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Published

25-04-2026

How to Cite

SURESHKUMAR, V., RAMALINGAM, K., & BALASUBRAMANIAN, A. (2026). FORMULATING A β CYCLODEXTRIN–DASATINIB INCLUSION COMPLEX BY KNEADING TO BOOST DISSOLUTION PERFORMANCE. International Journal of Applied Pharmaceutics, 18(4). https://doi.org/10.22159/ijap.2026v18i4.58035

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Articles In Press [Jul-Aug 2026]

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Copyright (c) 2026 VANITHA SURESHKUMAR, KOTHAI RAMALINGAM, ARUL BALASUBRAMANIAN

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