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Purpose <p>Curcumin (Cur), a hydrophobic polyphenol known for its antioxidant and anticancer properties, exhibits poor aqueous solubility and limited bioavailability. To enhance its therapeutic potential, a pH-responsive, chitosan-coated self-nanoemulsifying drug delivery system (Cur-SNEDDS-CS) was developed. The effects of varying chitosan concentrations (1, 2, and 4&#xa0;mg/mL) on its physicochemical characteristics, stability, in vitro drug release, and anticancer activity against MCF-7 cells were systematically investigated.</p> Methods <p>Formulations were characterized using dynamic Light scattering, zeta potential analysis, FTIR, TEM, encapsulation efficiency, and drug release profiles at pH levels of 5.4 and 7.4, and analyzed using kinetic modeling. The anticancer activity against MCF-7 cells was evaluated using the MTT assay method.</p> Results <p>Results showed that increasing chitosan concentration slightly increased globule size (16.3–19.9&#xa0;nm), PDI, and decreased zeta potential (-21 to -27 mV), while maintaining high encapsulation efficiencies (&gt; 93%). TEM confirmed successful chitosan coating, as evidenced by a core-shell morphology. The chitosan formulation at 2&#xa0;mg/mL exhibited the highest physical stability under stress conditions. In vitro release studies demonstrated that all Cur-SNEDDS-CS formulations exhibited strong pH-responsive behavior, with significantly higher drug release observed at acidic pH compared to neutral conditions. Kinetic analysis revealed that the release followed the Korsmeyer-Peppas model at both pH 5.4 and 7.4, with n values indicating a pH-responsive mechanism governed by diffusion and polymer relaxation. Importantly, MTT assay results showed that Cur-SNEDDS-CS exhibited significantly higher cytotoxicity against MCF-7 breast cancer cells (IC<sub>50</sub> = 1.638&#xa0;µg/mL) than free curcumin (IC<sub>50</sub> = 6.997&#xa0;µg/mL).</p> Conclusion <p>These findings highlight the versatility of Cur-SNEDDS-CS as a tumor-targeted nanocarrier system capable of enhancing curcumin’s anticancer efficacy.</p> Graphical Abstract <p></p>

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Chitosan-Coated Nanoemulsions for pH-Triggered Curcumin Release: Formulation Stability, Kinetic Behavior, and Anticancer Activity Against MCF-7 Cells

  • 期刊论文

  • 发表日期：

    2025年10月17日

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  • Winda Trisna Wulandari,
  • Mia Ledyastuti,
  • Marselina Irasonia Tan,
  • I Made Arcana

摘要

Purpose

Curcumin (Cur), a hydrophobic polyphenol known for its antioxidant and anticancer properties, exhibits poor aqueous solubility and limited bioavailability. To enhance its therapeutic potential, a pH-responsive, chitosan-coated self-nanoemulsifying drug delivery system (Cur-SNEDDS-CS) was developed. The effects of varying chitosan concentrations (1, 2, and 4 mg/mL) on its physicochemical characteristics, stability, in vitro drug release, and anticancer activity against MCF-7 cells were systematically investigated.

Methods

Formulations were characterized using dynamic Light scattering, zeta potential analysis, FTIR, TEM, encapsulation efficiency, and drug release profiles at pH levels of 5.4 and 7.4, and analyzed using kinetic modeling. The anticancer activity against MCF-7 cells was evaluated using the MTT assay method.

Results

Results showed that increasing chitosan concentration slightly increased globule size (16.3–19.9 nm), PDI, and decreased zeta potential (-21 to -27 mV), while maintaining high encapsulation efficiencies (> 93%). TEM confirmed successful chitosan coating, as evidenced by a core-shell morphology. The chitosan formulation at 2 mg/mL exhibited the highest physical stability under stress conditions. In vitro release studies demonstrated that all Cur-SNEDDS-CS formulations exhibited strong pH-responsive behavior, with significantly higher drug release observed at acidic pH compared to neutral conditions. Kinetic analysis revealed that the release followed the Korsmeyer-Peppas model at both pH 5.4 and 7.4, with n values indicating a pH-responsive mechanism governed by diffusion and polymer relaxation. Importantly, MTT assay results showed that Cur-SNEDDS-CS exhibited significantly higher cytotoxicity against MCF-7 breast cancer cells (IC50 = 1.638 µg/mL) than free curcumin (IC50 = 6.997 µg/mL).

Conclusion

These findings highlight the versatility of Cur-SNEDDS-CS as a tumor-targeted nanocarrier system capable of enhancing curcumin’s anticancer efficacy.

Graphical Abstract