Nilotinib-loaded hydroxy propyl β-cyclodextrin nanosponges for improved oral bioavailability in chronic myeloid leukemia therapy.

Authors

Bhagya Buela Gudipalli, Surendra Av, Ramakrishna Kakarla, Datta Maroti Pawde, Avinash Kumar G, Udaykumar Thummala, Shailendra Singh, Chakravarthi Guntupalli, Buchi N Nalluri, Sona Muthu Madaswamy, Kasi Viswanadh Matte

Published in

Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences. Volume 34. Issue 2. Aug 12, 2026. Epub Aug 12, 2026.

Abstract

Poor aqueous solubility and low permeability limit the oral bioavailability of Nilotinib, a second-generation tyrosine kinase inhibitor used in chronic myeloid leukemia. Nanosponges prepared using cyclodextrin derivatives offer a scalable and efficient platform for enhancing solubility, controlling release, and improving bioavailability. Therefore, this study aimed to formulate Nilotinib-loaded hydroxypropyl β-cyclodextrin nanosponges to enhance oral absorption.
Hydroxypropyl β-cyclodextrin nanosponges were synthesized using diphenyl carbonate as a cross-linker. Box-Behnken Design, under a Quality-by-Design framework, was applied to optimize critical parameters including mixing speed, reaction time, and molar ratio. The optimized formulation was characterized for particle size, zeta potential, entrapment efficiency, morphology, compatibility, drug release, permeability, and pharmacokinetic performance in rats.
The optimized nanosponges showed a particle size of 203.1 ± 3.1 nm, zeta potential of - 24.0 ± 2.55 mV, and entrapment efficiency of 66.88 ± 2.66%. SEM confirmed a uniform porous structure. In vitro release and permeability demonstrated enhanced performance compared to pure drug. Pharmacokinetic evaluation revealed a 2.68-fold increase in AUC₀₋ₜ, indicating improved oral bioavailability.
Nilotinib-loaded hydroxypropyl β-cyclodextrin nanosponges significantly enhanced dissolution, permeability, and systemic exposure, suggesting a promising and scalable strategy to improve the therapeutic performance of Nilotinib.

PMID:
42584826
Bibliographic data and abstract were imported from PubMed on 13 Aug 2026.

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