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Background <p>To develop chitosan-stabilized lycopene nanoparticles (CSLN) as a dual-drug delivery system for doxorubicin and paclitaxel, and to evaluate their physicochemical characteristics, drug release kinetics, cytotoxicity, and gene expression effects against oral squamous cell carcinoma.</p> Materials and Methods <p>Chitosan (degree of deacetylation: 86.4%) was extracted from squid pen waste, and lycopene (yield: 91%) was isolated from tomato pulp. Chitosan nanoparticles were synthesized using the ionic gelation method. Characterization was performed by Fourier transform infrared spectroscopy and high-resolution scanning electron microscopy. Drug loading, entrapment efficiency, and in vitro release (pH 5.0 and 7.4) were spectrophotometrically quantified. Cytotoxicity on SCC-9 cells was assessed using MTT assay, and expression of BOX, BCL-2, Caspase-3, Cyclin D1, and p53 was analyzed via qRT-PCR.</p> Results <p>CSLN showed an average particle size of 137.2 ± 4.3&#xa0;nm and a zeta potential of + 21.3&#xa0;mV. The entrapment efficiencies were 74.6% for doxorubicin and 68.2% for paclitaxel. At pH 5.0, the 48-h cumulative release reached 78.4% (DOX) and 71.2% (PTX). IC<sub>50</sub> values were 18.6&#xa0;μg/mL (DOX-LCN) and 21.4&#xa0;μg/mL (PTX-LCN). Gene expression showed upregulation of p53 (+ 3.1-fold), BAX (+ 4.5-fold), and Caspase-3 (+ 2.8-fold), and downregulation of BCL-2 (− 3.9-fold) and Cyclin D1 (− 2.7-fold).</p> Conclusion <p>CSLN provides efficient, pH-sensitive dual-drug delivery with strong cytotoxic and gene-modulatory effects, indicating a promising potential for targeted oral cancer therapy.</p>

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In Vitro Evaluation of Chitosan-Stabilized Lycopene Nanoparticles for Antioxidant and Anticancer Drug Delivery

  • 期刊论文

  • 发表日期：

    2025年9月11日

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  • Senthil Rethinam

摘要

Background

To develop chitosan-stabilized lycopene nanoparticles (CSLN) as a dual-drug delivery system for doxorubicin and paclitaxel, and to evaluate their physicochemical characteristics, drug release kinetics, cytotoxicity, and gene expression effects against oral squamous cell carcinoma.

Materials and Methods

Chitosan (degree of deacetylation: 86.4%) was extracted from squid pen waste, and lycopene (yield: 91%) was isolated from tomato pulp. Chitosan nanoparticles were synthesized using the ionic gelation method. Characterization was performed by Fourier transform infrared spectroscopy and high-resolution scanning electron microscopy. Drug loading, entrapment efficiency, and in vitro release (pH 5.0 and 7.4) were spectrophotometrically quantified. Cytotoxicity on SCC-9 cells was assessed using MTT assay, and expression of BOX, BCL-2, Caspase-3, Cyclin D1, and p53 was analyzed via qRT-PCR.

Results

CSLN showed an average particle size of 137.2 ± 4.3 nm and a zeta potential of + 21.3 mV. The entrapment efficiencies were 74.6% for doxorubicin and 68.2% for paclitaxel. At pH 5.0, the 48-h cumulative release reached 78.4% (DOX) and 71.2% (PTX). IC50 values were 18.6 μg/mL (DOX-LCN) and 21.4 μg/mL (PTX-LCN). Gene expression showed upregulation of p53 (+ 3.1-fold), BAX (+ 4.5-fold), and Caspase-3 (+ 2.8-fold), and downregulation of BCL-2 (− 3.9-fold) and Cyclin D1 (− 2.7-fold).

Conclusion

CSLN provides efficient, pH-sensitive dual-drug delivery with strong cytotoxic and gene-modulatory effects, indicating a promising potential for targeted oral cancer therapy.