What question did this study set out to answer?

Develop a novel nanoformulation of silybin and curcumin to enhance their hepatoprotective and anticancer effects.

February 12, 2026Journal of Pharmaceutical Innovation1 citationsOpen Access

Silybum Marianum-based Nanoformulations for Enhanced Hepatoprotective and Anticancer Activity

SMSamar M. Mahgoub AAAbdullah S. Alawam HRHassan A. RudayniImam Mohammad ibn Saud Islamic University

Key Points

Develop a novel nanoformulation of silybin and curcumin to enhance their hepatoprotective and anticancer effects.
Coencapsulation of silybin and curcumin with Silybum marianum seed extract.
Characterization of particle size, zeta potential, and encapsulation efficiency.
Molecular docking studies on interactions with proteins related to cancer and inflammation.
Assessment of antimicrobial activity against mastitis pathogens.
Cytotoxicity evaluation in MCF-7 and HepG2 cell lines.
Mean particle size of the nanoformulation was 191.00 ± 2.25 nm.
High encapsulation efficiencies: silybin (85.5 ± 2.1%) and curcumin (82.3 ± 1.8%).
Cumulative release of 98.1% for silybin and 89.1% for curcumin over 48 hours.
Strong binding affinity of silybin with AKT1 (−11.9 kcal/mol).
IC50 of 81.11 ± 1.95 µg/mL in MCF-7 cells, demonstrating anticancer efficacy.

Abstract

Abstract Purpose The poor solubility, low bioavailability, and rapid degradation of bioactive compounds such as silybin and curcumin limit their therapeutic potential. This study aims to develop a novel nanoformulation by coencapsulating silybin and curcumin with Silybum marianum seed extract, a natural encapsulant, to increase their stability, bioavailability, and therapeutic efficacy for hepatoprotection and anticancer applications. Methods Silybin and curcumin were encapsulated via a nanoprecipitation method. The formulation was characterized for its particle size, zeta potential, encapsulation efficiency, and in vitro release kinetics. Molecular docking studies were conducted to evaluate interactions with key proteins (Nrf2, COX-2, TNF-α, P53, and AKT1) involved in oxidative stress, inflammation, and cancer. Antimicrobial activity was assessed against mastitis-related pathogens via the agar well diffusion and broth dilution methods. Cytotoxicity was evaluated in the MCF-7 (breast cancer) and HepG2 (liver cancer) cell lines via the MTT assay. Results The nanoformulation resulted in a mean particle size of 191.00 ± 2.25 nm, a zeta potential of −32.03 ± 1.63 mV, and high encapsulation efficiencies for silybin (85.5 ± 2.1%) and curcumin (82.3 ± 1.8%). Sustained release profiles were observed, with 98.1% and 89.1% cumulative release for silybin and curcumin, respectively, over 48 h. Molecular docking revealed strong binding affinities, particularly for silybin with AKT1 (−11.9 kcal/mol) and for curcumin with COX-2 (−8.4 kcal/mol). The formulation demonstrated enhanced antimicrobial activity, with a minimum inhibitory concentration (MIC) of 20.90 ± 5.20 µg/mL against E. coli , and superior anticancer efficacy, with an IC50 of 81.11 ± 1.95 µg/mL in MCF-7 cells. Conclusion This study presents a novel, natural nanoformulation with dual hepatoprotective and anticancer potential. The use of Silybum marianum seed extract as both a bioactive encapsulant and a therapeutic synergist offers a sustainable and effective alternative to synthetic drug delivery systems, highlighting its potential for clinical applications in liver diseases and cancer therapy. Graphical Abstract

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