Designing and Characterization of Docetaxel Loaded Nanoparticles with Piperine

Objective: The main objective of this research was to develop a novel formulation with an herbal bioenhancer to boost the bioavailability of an anticancer drug that was poorly soluble in water and overcome its limitations of short half-life.

Methods: Eudragit RLPO was used as a polymer in an emulsification solvent evaporation process to generate Docetaxel loaded bioenhancer (Piperine) nanoparticles and to evaluate its parameters.

Results: The study demonstrated that encapsulating Docetaxel with herbal bioenhancers (Piperine) in a nanoparticle system effectively enhanced its in vitro release profile. The particle size range (142 to 189 nm) is optimal range for enhanced cellular uptake and improved bioavailability for nanoparticle drug delivery, and the drug release from all batches was significant, with a release percentage ranging from 83.69% to 96.44% over 24 hours. This indicates a controlled release profile, which is desirable for maintaining therapeutic drug levels over an extended period.

The release data adhered to Fick's law of diffusion, suggesting that the drug release mechanism is diffusion-controlled. Higuchi's model best described the release kinetics, indicating that the release rate is proportional to the square root of time, which is typical for systems where the drug release is controlled by diffusion through a polymer matrix.

Conclusion: The study demonstrated that encapsulating Docetaxel with herbal bioenhancers (Piperine) in a nanoparticle system effectively enhanced its in vitro release profile. The particle size range (142 to 189 nm) is optimal for nanoparticle drug delivery, and the release kinetics following Higuchi’s model confirm the controlled release mechanism. The significant finding that higher amounts of Piperine enhance drug release rates underscores the potential of using bioenhancers to improve the bioavailability of poorly water-soluble drugs like Docetaxel.

These promising in vitro results pave the way for further in vivo pharmacokinetic and cytotoxicity studies to fully assess the therapeutic potential and bioavailability improvements provided by this novel formulation.