What question did this study set out to answer?

The aim is to formulate and evaluate PLGA nanoparticles for targeted delivery of curcumin in breast cancer therapy.

May 10, 2026Open Access

Formulation, Characterisation, and In-Vitro Evaluation of Chitosan-PEG Conjugated PLGA Nanoparticles for Targeted Curcumin Delivery in Breast Cancer Therapy

Key Points

The aim is to formulate and evaluate PLGA nanoparticles for targeted delivery of curcumin in breast cancer therapy.
Formulation of six PLGA-based nanoparticle formulations incorporating curcumin with varying chitosan coating levels (5%, 10%, 15% w/w) and PEG conjugation.
In-vitro characterization included drug encapsulation efficiency, particle size measurement, release studies at pH 7.4 and pH 5.0, and cell viability assay against MCF-7 cells.
Nanoparticles were prepared using nanoprecipitation method and characterized by techniques such as DLS, FTIR, and TEM.
F6 formulation achieved the highest encapsulation efficiency at 84.1% and smallest mean particle size of 168 nm.
The zeta potential was -34.8 mV, and the lowest IC50 against MCF-7 cells was 62.6 µg/mL.
In-vitro release studies showed sustained release over 24 hours with enhanced release at pH 5.0.

Abstract

Curcumin (diferuloylmethane), a hydrophobic polyphenol derived from the rhizome of Curcuma longa, exhibits well-documented anti-tumour, anti-inflammatory, and antioxidant bioactivities across multiple cancer cell lines, including MCF-7 human breast adenocarcinoma. However, its therapeutic translation is severely impeded by poor aqueous solubility (< 1 µg/mL at physiological pH), rapid metabolic degradation, and systemic bioavailability below 1% following oral administration — collectively limiting its achievable tumour-site concentration to sub-therapeutic levels. Nanoparticulate encapsulation within biodegradable polymer matrices offers a rational strategy to overcome these limitations by protecting the hydrophobic payload from premature degradation, improving colloidal dispersion, and enabling surface functionalisation for receptor-mediated tumour targeting. This study reports the formulation, physicochemical characterisation, and in-vitro evaluation of six PLGA-based nanoparticle (NP) formulations incorporating curcumin at varying chitosan (CS) coating levels (5%, 10%, 15% w/w) and polyethylene glycol (PEG) conjugation, with a ternary formulation (F6) combining 10%CS and PEG surface modification. Nanoparticles were prepared by nanoprecipitation method with characterisation encompassing drug encapsulation efficiency (EE%), dynamic light scattering (DLS) particle size and zeta potential, polydispersity index (PDI), in-vitro drug release at pH 7.4 and pH 5.0 (simulating tumour microenvironment), FTIR spectroscopy, differential scanning calorimetry (DSC), transmission electron microscopy (TEM) structural analysis, MTT cell viability assay against MCF-7 cells, and colloidal stability study over 90 days. The ternary F6 formulation achieved the highest encapsulation efficiency (84.1%), smallest mean particle size (168 nm), most negative zeta potential (-34.8 mV), and lowest IC50 against MCF-7 cells (62.6 µg/mL versus 88.4 µg/mL for plain PLGA NPs and 42.8 µg/mL for free curcumin at 24h). In-vitro release studies confirmed sustained release over 24 hours with pH-responsive enhanced release at pH 5.0, simulating tumour microenvironment conditions. Haemolysis assay confirmed biocompatibility at therapeutic concentrations (haemolysis below 5% at 1 mg/mL). The F6 ternary formulation is recommended as an optimised platform for further in-vivo evaluation in breast cancer xenograft models.

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