Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2026
Nilotinib-loaded hydroxy propyl β-cyclodextrin nanosponges for improved oral bioavailability in chronic myeloid leukemia therapy.
СтатьяНазвание и аннотация: Перевод в очереди
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Gudipalli Bhagya Buela, Av Surendra, Kakarla Ramakrishna, Pawde Datta Maroti, G Avinash Kumar, Thummala Udaykumar, Singh Shailendra, Guntupalli Chakravarthi, Nalluri Buchi N, Madaswamy Sona Muthu, Matte Kasi Viswanadh
Аннотация
OBJECTIVE: 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.
METHODS: 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.
RESULTS: 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.
CONCLUSION: 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.
METHODS: 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.
RESULTS: 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.
CONCLUSION: 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.