Background: A novel formulation for cabazitaxel loaded HSA nanoparticle (Cbz-NPs) with non-crosslinking
agent participation was reported in this study.
Objective: A simple method through unfolding of HSA self-assembling nanoparticle for cabazitaxel (Cbz) overcomes
the drawbacks of Cbz with high toxicity, poor solubility and low tissue specificity, and avoids side effects of
polysorbate 80 which is commonly used for dissolving Cbz.
Method: The optimum condition was obtained by Response surface methodology (RSM). The NPs were analyzed by
differential scanning calorimetry (DSC) and drug release in vitro was also determined. Furthermore, cytotoxicity,
cellular uptake were assessed.
Results: The experimental encapsulation efficacy (EE) is 52.95%, which is close to the predicted value of 62.44%,
indicating the correct prediction, and the nanoscale-sized particles enhanced permeability and retention (EPR) effect.
Differential scanning calorimetry (DSC) demonstrates an amorphous state of cabazitaxel-NPs, and a sustained release
was found in vitro drug release. Human prostate cancer lines PC3 and Human Lung Cancer line A549 were employed
for cytotoxicity study by the MTT test. Single solvent with polysorbate 80 showed serious cytotoxicity with the cell
viability of only 80% while no toxicity was found in drug-free nanoparticles. Fluorescence intensity of FITC-HSA
nanoparticles encapsulating Cbz increased with the incubation time. The cellular localizatiton of cabazitaxel-NPs was
observed by confocal microscopy.
Conclusion: Cbz-NPs may be considered as a viable opportunity for anticancer drug delivery.