Cabozantinib-phospholipid complex for enhanced solubility, bioavailability, and reduced toxicity in liver cancer.

ABSTRACT:

Aims

To enhance the therapeutic potential of Cabozantinib (CBZ), a tyrosine kinase inhibitor with limited water solubility, low bioavailability, and high toxicity, by developing a Cabozantinib-Phospholipid Complex (CBZ-PLS).

Materials & methods

CBZ-PLS was formulated using solvent evaporation with a Box-Behnken design and characterized using various techniques to confirm molecular interactions. Solubility, in vitro release, pharmacokinetics, and toxicity were evaluated. Cytotoxic effects on HepG2 cell lines were also assessed.

Results

CBZ-PLS exhibited a 126-fold increase in solubility and enhanced CBZ release in vitro. Pharmacokinetic studies on Wistar rats demonstrated a 1.58-fold increase in bioavailability, while acute toxicity studies confirmed biocompatibility.

SUBMITTER: Patil J 

PROVIDER: S-EPMC11703380 | biostudies-literature | 2025 Jan

REPOSITORIES: biostudies-literature