Erlotinib loaded chitosan nanoparticles: Formulation, physicochemical characterization and cytotoxic potential

Area of Science:

• Nanotechnology
• Pharmaceutical Sciences
• Oncology

Background:

• Cancer remains a leading global cause of mortality, with over 10 million new cases annually.
• Effective drug delivery systems are crucial for improving cancer therapy outcomes.
• Erlotinib is a targeted therapy for certain cancers, but its delivery can be optimized.

Purpose of the Study:

• To prepare and evaluate erlotinib-loaded chitosan nanoparticles (NPs) for anticancer potential.
• To optimize nanoparticle formulation using Box-Behnken design.
• To assess the in vitro anticancer activity and stability of the developed NPs.

Main Methods:

• Erlotinib-loaded chitosan NPs were synthesized using the ionic gelation method and spray drying technique.
• Box-Behnken design was employed to optimize formulation variables.
• Particle size, loading capacity, entrapment efficiency, drug release, and in vitro cytotoxicity were evaluated.

Main Results:

• The optimized batch (SNP-9) exhibited a high loading capacity (74.45%) and entrapment efficiency (43%) with a particle size of 170.2 nm.
• ANOVA confirmed the significance of formulation variables on nanoparticle characteristics.
• SNP-9 demonstrated sustained drug release and potent in vitro anticancer activity against A549 lung cancer cells (IC50 = 4.41 μM).
• The optimized formulation remained stable for six months.

Conclusions:

• Erlotinib-loaded chitosan nanoparticles were successfully prepared and optimized using spray drying.
• The developed nanoparticles possess suitable physicochemical properties and significant in vitro anticancer activity.
• These nanoparticles offer a promising approach for improved cancer therapy.