Cabozantinib Loaded DSPE-PEG2000 Micelles as Delivery System: Formulation, Characterization and Cytotoxicity Evaluation
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Updated: Apr 17, 2026
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Qiuhong Yang1, Ryan Moulder K2, Mark S Cohen3
1Department of Pharmaceutical Chemistry, University of Kansas, Lawrence, KS, USA.
Abstract:
Cabozantinib, a potent pan-tyrosine kinase inhibitor, has been reported to provide enhanced antitumor efficacy by simultaneously inhibiting both MET and VEGF pathways, which are critical to tumor angiogenesis, survival and migration. It's very poor water solubility prevents its administration by the intravenous route, which may be important in patients unable to take the drug orally. In this study, we developed an efficient PEG-lipid-based polymeric micelle formulation with enhanced drug solubility and stability for cabozantinib delivery. DSPE-PEG2000 micelles encapsulating cabozantinib were prepared by a thin-film rehydration method followed by a lyophilization process to generate the dry dosage form. The average hydrodynamic diameter of freshly prepared micelles was 11 nm with a narrow size distribution, and the dry micelle cake could be fully reconstituted by rehydration. Approximately 75% of the drug was encapsulated into the lyophilized cake, and a sustained drug release profile was observed in simulated normal physiological release medium. Compared with the free cabozantinib solution, the drug-loaded micelles displayed significantly enhanced intracellular accumulation and cytotoxicity in human glioblastoma cancer cells and non-small lung cancer cells. These results suggest that the micellar formulation of cabozantinib may serve as a promising nanocarrier in anticancer treatments.
Insights
This study developed a novel micelle formulation for cabozantinib, improving its solubility and enabling potential intravenous delivery. The new formulation demonstrated enhanced cancer cell uptake and effectiveness against glioblastoma and lung cancer cells.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Pharmacology
Background:
- Cabozantinib is a tyrosine kinase inhibitor targeting MET and VEGF pathways crucial for tumor growth.
- Poor water solubility limits cabozantinib's administration, particularly for patients unable to take oral medication.
Purpose of the Study:
- To develop an efficient PEG-lipid-based polymeric micelle formulation for enhanced cabozantinib delivery.
- To improve cabozantinib solubility, stability, and enable potential intravenous administration.
Main Methods:
- Cabozantinib was encapsulated into DSPE-PEG2000 micelles using a thin-film rehydration method.
- Micelles were lyophilized to create a stable, reconstitutable dry dosage form.
- Drug encapsulation efficiency, particle size, drug release, cellular accumulation, and cytotoxicity were evaluated.
Main Results:
- The micellar formulation achieved approximately 75% drug encapsulation efficiency.
- The micelles exhibited sustained drug release in a simulated physiological medium.
- Drug-loaded micelles showed significantly enhanced intracellular accumulation and cytotoxicity in glioblastoma and non-small cell lung cancer cells compared to free cabozantinib.
Conclusions:
- The developed micellar formulation effectively enhances cabozantinib solubility and stability.
- This nanocarrier system shows promise for improved anticancer treatment delivery, particularly via intravenous routes.
- The formulation warrants further investigation for clinical applications in cancer therapy.
