Synthesis, Characterization and Controlled Release Evaluation of PLGA–Chitosan Polymeric Nanoparticles for Targeted Doxorubicin Delivery in Cancer Therapy

Abstract

Cancer therapy using conventional chemotherapeutic agents is often associated with several limitations, including non-specific drug distribution, systemic toxicity, poor bioavailability, and rapid drug clearance. Doxorubicin, a widely used anti-cancer drug, exhibits significant therapeutic potential; however, its clinical application is restricted due to severe side effects and inadequate targeting efficiency. The present study focuses on the synthesis, characterization, and controlled release evaluation of PLGA–Chitosan polymeric nanoparticles for targeted delivery of Doxorubicin in cancer therapy. Poly(lactic-co-glycolic acid) (PLGA) and Chitosan were selected due to their biodegradable, biocompatible, and controlled release properties. Nanoparticles were synthesized using an optimized nano-precipitation technique followed by Doxorubicin encapsulation within the polymeric matrix.

The developed nanoparticles were characterized using Fourier Transform Infrared Spectroscopy (FTIR), Dynamic Light Scattering (DLS), Zeta potential analysis, Scanning Electron Microscopy (SEM), and Transmission Electron Microscopy (TEM). FTIR analysis confirmed successful drug encapsulation and polymer–drug interaction, while DLS results demonstrated nanoscale particle size distribution with acceptable polydispersity index and surface stability. SEM and TEM analysis revealed spherical and uniformly dispersed nanoparticles. Drug loading capacity and entrapment efficiency studies indicated efficient incorporation of Doxorubicin within the nanoparticle system.

In-vitro drug release studies demonstrated a controlled and sustained release profile over an extended period, following diffusion-controlled release kinetics. The developed nanoformulation exhibited significantly improved release behaviour compared to conventional Doxorubicin. Cytotoxicity analysis using cancer cell lines revealed enhanced anti-cancer activity and improved cellular uptake of the nanoparticle formulation, resulting in reduced IC₅₀ values and enhanced therapeutic efficiency. The PLGA–Chitosan nanoparticle system also showed potential for minimizing systemic toxicity through targeted and sustained drug delivery.