Related Experiment Video
Updated: Aug 14, 2026
Encapsulation of Cancer Therapeutic Agent Dacarbazine Using Nanostructured Lipid Carrier
Published on: April 26, 2016
Nilotinib-loaded hydroxy propyl β-cyclodextrin nanosponges for improved oral bioavailability in chronic myeloid
Bhagya Buela Gudipalli1, Surendra Av1, Ramakrishna Kakarla1
1KL College of Pharmacy, Koneru Lakshmaiah Education Foundation, Vijayawada, India.
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.
Insights
Nilotinib-loaded hydroxypropyl β-cyclodextrin nanosponges significantly improved oral absorption and bioavailability. This formulation offers a promising strategy to enhance the therapeutic efficacy of Nilotinib for chronic myeloid leukemia treatment.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Nanotechnology
Background:
- Nilotinib, a tyrosine kinase inhibitor, faces challenges in oral bioavailability due to poor solubility and permeability.
- Cyclodextrin-based nanosponges present a viable approach to overcome these limitations by enhancing drug solubility and controlling release.
Purpose of the Study:
- To formulate and characterize Nilotinib-loaded hydroxypropyl β-cyclodextrin nanosponges.
- To evaluate the potential of these nanosponges in improving the oral absorption and therapeutic performance of Nilotinib.
Main Methods:
- Hydroxypropyl β-cyclodextrin nanosponges were synthesized using diphenyl carbonate and optimized via Box-Behnken Design.
- Characterization included particle size, zeta potential, entrapment efficiency, morphology (SEM), drug release, permeability, and in vivo pharmacokinetics in rats.
Main Results:
- Optimized nanosponges exhibited favorable characteristics: 203.1 nm particle size, -24.0 mV zeta potential, and 66.88% entrapment efficiency.
- Enhanced in vitro dissolution and permeability were observed compared to pure Nilotinib.
- Pharmacokinetic studies showed a 2.68-fold increase in AUC₀₋ₜ, indicating significantly improved oral bioavailability.
Conclusions:
- Nilotinib-loaded hydroxypropyl β-cyclodextrin nanosponges demonstrate a scalable and effective strategy for enhancing drug dissolution, permeability, and systemic exposure.
- This formulation holds significant promise for improving the therapeutic outcomes in patients treated with Nilotinib for chronic myeloid leukemia.
