Genistein solid dispersion: preparation, physical-chemical characters and anti-oxidant properties

Xiaofei Liu , Yang Liu , Hongyue Wang , Xiangrong Zhang

Journal of Polyphenols ›› 2025, Vol. 7 ›› Issue (3) : 112 -126.

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Journal of Polyphenols ›› 2025, Vol. 7 ›› Issue (3) : 112 -126.
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Genistein solid dispersion: preparation, physical-chemical characters and anti-oxidant properties

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Abstract

The aim of this study was to enhance the applicability of genistein (GEN) and investigate genistein solid dispersion (GEN-SD). The optimal process parameters were determined as follows: anhydrous ethanol volume ratio of 4:1, ultrasonication time of 30 min, rotary evaporation temperature of 50 °C, and a drug-to-carrier mass ratio of 1:7. The results of the dissolution and solubility experiments showed that the dissolution rate and solubility of the optimized solid dispersion were significantly improved compared to pure GEN. Comprehensive characterization of the GEN-SD using X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and Fourier transform infrared spectroscopy clarified variations in crystalline form, thermal properties, and microscopic morphology. Antioxidant experiments showed that GEN- SD exhibited antioxidant activity and could effectively scavenge various free radicals. Stability studies demonstrated that GEN-SD was stable at a high temperature of 60 ℃ and a light intensity of 4500 lx.

Keywords

Genistein / Solid dispersion / Polyvinylpyrrolidone K30 / Antioxidant

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Xiaofei Liu, Yang Liu, Hongyue Wang, Xiangrong Zhang. Genistein solid dispersion: preparation, physical-chemical characters and anti-oxidant properties. Journal of Polyphenols, 2025, 7(3): 112-126 DOI:

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Acknowledgement

This study was supported by department of Education of Liaoning Province (Natural Science, Strategic Industrialization Project (LJ212410163061).

References

[1]

Sharifi-Rad J, Quispe C, Imran M, et al. Genistein: An Integrative Overview of Its Mode of Action, Pharmacological Properties, and Health Benefits[J]. Oxid Med Cell Longev, 2021, 2021: 3268136.

[2]

Bernatoniene J, Kazlauskaite JA, Kopustinskiene DM. Pleiotropic Effects of Isoflavones in Inflammation and Chronic Degenerative Diseases[J]. Int J Mol Sci, 2021, 22(11): 5656.

[3]

Panche AN, Diwan AD, Chandra SR. Flavonoids: an overview[J]. J Nutr Sci, 2016, 5: e47.

[4]

Goh YX, Jalil J, Lam KW, et al. Genistein: A Review on its Anti-Inflammatory Properties[J]. Front Pharmacol, 2022, 13: 820969.

[5]

Mei J, Chen X, Liu J, et al. A Biotransformation Process for Production of Genistein from Sophoricoside by a Strain of Rhizopus oryza[J]. Sci Rep, 2019, 9(1): 6564.

[6]

Jeong JW, Lee HH, Han MH, et al. Anti-inflammatory effects of genistein via suppression of the toll-like receptor 4-mediated signaling pathway in lipopolysaccharide- stimulated BV2 microglia[J]. Chem Biol Interact, 2014, 212: 30-39.

[7]

Michael McClain R, Wolz E, Davidovich A, et al. Genetic toxicity studies with genistein[J]. Food Chem Toxicol, 2006, 44(1): 42-55.

[8]

Liu Q, Zhang R, Chen Y, et al. Dietary Flavonoid Intake and Risk of Mild Cognitive Impairment in the Elderly: A Case-Control Study[J]. Nutr Metab Insights, 2024, 17: 11786388241283779.

[9]

Ronchetti S, Labombarda F, Del Core J, et al. The phytoestrogen genistein improves hippocampal neurogenesis and cognitive impairment and decreases neuroinflammation in an animal model of metabolic syndrome[J]. J Neuroendocrinol, 2025, 37(2): e13480.

[10]

Jaiswal KS, Malka O, Shauloff N, et al. Genistein carbon dots exhibit antioxidant and anti-inflammatory effects in vitro[J]. Colloids Surf B Biointerfaces, 2023, 223: 113173.

[11]

Tang H, Wang S, Li X, et al. Prospects of and limitations to the clinical applications of genistein[J]. Discov Med, 2019, 27(149): 177-188.

[12]

Qiu C, Zhang Y, Fan Y, et al. Solid Dispersions of Genistein via Solvent Rotary Evaporation for Improving Solubility, Bioavailability, and Amelioration Effect in HFD-Induced Obesity Mice[J]. Pharmaceutics, 2024, 16(3): 306.

[13]

Vu QL, Fang CW, Suhail M, et al. Enhancement of the Topical Bioavailability and Skin Whitening Effect of Genistein by Using Microemulsions as Drug Delivery Carriers[J]. Pharmaceuticals (Basel), 2021, 14(12): 1233.

[14]

Shete VS, Telange DR, Mahajan NM, et al. Development of phospholipon®90H complex nanocarrier with enhanced oral bioavailability and anti-inflammatory potential of genistein[J]. Drug Deliv, 2023, 30(1): 2162158.

[15]

Shao Y, Zhao XX, Guo M, et al. Delivery Mechanism of the Pharmaceutical Complex of Genistein-Adenine Based on Spectroscopic and Molecular Modelling at Atomic Scale[J]. Chem Biodivers, 2021, 18(2): e2000944.

[16]

Vo CL, Park C and Lee BJ. Current trends and future perspectives of solid dispersions containing poorly water- soluble drugs[J]. Eur J Pharm Biopharm, 2013, 85(3 Pt B): 799-813.

[17]

Baghel S, Cathcart H, O’Reilly NJ. Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs[J]. J Pharm Sci, 2016, 105(9): 2527-2544.

[18]

Shukla D, Kaur S, Singh A, et al. Enhanced antichemobrain activity of amino acid assisted ferulic acid solid dispersion in adult zebrafish (Danio rerio)[J]. Drug Deliv Transl Res, 2024, 14(12): 3422-3437.

[19]

Wang C, Liu X, Zhao R, et al. The Amorphous Solid Dispersion of Chrysin in Plasdone(®) S630 Demonstrates Improved Oral Bioavailability and Antihyperlipidemic Performance in Rats[J]. Pharmaceutics, 2023, 15(10): 2378.

[20]

Assim Haq S, Paudwal G, Banjare N, et al. Sustained release polymer and surfactant based solid dispersion of andrographolide exhibited improved solubility, dissolution, pharmacokinetics, and pharmacological activity[J]. Int J Pharm, 2024, 651: 123786.

[21]

Hiew TN, Solomos MA, Kafle P, et al. The importance of surface composition and wettability on the dissolution performance of high drug loading amorphous dispersion formulations[J]. J Pharm Sci, 2025, 114(1): 289-303.

[22]

Huang H, Zhang Y, Hu C. Study on the crystallinity of PEG on the crystalline size of flavonoids in a crystalline dispersion system[J]. Eur J Pharm Biopharm, 2024, 205: 114536.

[23]

Liang H, Sun C, Feng Z, et al. Study on Integrated Pharmacokinetics of the Component-Based Chinese Medicine of Ginkgo biloba Leaves Based on Nanocrystalline Solid Dispersion Technology[J]. Int J Nanomedicine, 2022, 17: 4039-4057.

[24]

Ye Q, Li T, Li J, et al. Development and evaluation of tea polyphenols loaded water in oil emulsion with zein as stabilizer[J]. J Drug Delivery Sci Tech, 2020, 56: 101528.

[25]

Li S, Zhang Z, Gu W, et al. Hot Melt Extruded High-Dose Amorphous Solid Dispersions Containing Lumefantrine and Soluplus[J]. Int J Pharm, 2024, 665: 124676.

[26]

Zhu J, Xu Z, Liu X. Chemical composition, antioxidant activities, and enzyme inhibitory effects of Lespedeza bicolour Turcz. essential oil[J]. J Enzyme Inhib Med Chem, 2025, 40(1): 2460053.

[27]

Zhang T, Wang H, Hu H, et al. Composite film based on carboxymethyl cellulose and gellan gum with honokiol- β-cyclodextrin inclusion complex: Characterization and application in strawberry preservation[J]. Int J Biol Macromol, 2024, 282(Pt 1): 136740.

[28]

Shimada O, Yasuda H. Hydroxyl radical scavenging action of tinoridine[J]. Agents Actions, 1986, 19(3-4): 208-214.

[29]

Kurakula M, Rao G. Pharmaceutical assessment of polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a spotlight on COVID-19 inhibition[J]. J Drug Deliv Sci Technol, 2020, 60: 102046.

[30]

Markeev VB, Tishkov SV, Vorobei AM, et al. Modeling of the Aqueous Solubility of N-butyl-N-methyl-1-phenylpyrrolo[1,2-a] pyrazine-3-carboxamide: From Micronization to Creation of Amorphous-Crystalline Composites with a Polymer[J]. Polymers (Basel), 2023, 15(20): 4136.

[31]

Gera T, Nagy E, Smausz T, et al. Application of pulsed laser ablation (PLA) for the size reduction of non-steroidal anti-inflammatory drugs (NSAIDs)[J]. Sci Rep, 2020, 10(1): 15806.

[32]

Ishtiaq M, Manzoor H, Khan IU, et al. Curcumin-loaded soluplus® based ternary solid dispersions with enhanced solubility, dissolution and antibacterial, antioxidant, anti-inflammatory activities[J]. Heliyon, 2024, 10(14): e34636.

[33]

Li Y, Wei Q, Su J, et al. Encapsulation of astaxanthin in OSA-starch based amorphous solid dispersions with HPMCAS-HF/Soluplus® as effective recrystallization inhibitor[J]. Int J Biol Macromol, 2024, 279(Pt 1): 135421.

[34]

Khuanekkaphan M, Netsomboon K, Fristiohady A, et al. Development of Quercetin Solid Dispersion-Loaded Dissolving Microneedles and In Vitro Investigation of Their Anti-Melanoma Activities[J]. Pharmaceutics, 2024, 16(10): 1276.

[35]

Zhou Z, Chen J, Zhang ZX, et al. Solubilization of luteolin in PVP40 solid dispersion improves inflammation-induced insulin resistance in mice[J]. Eur J Pharm Sci, 2022, 174: 106188.

[36]

Jangid AK, Solanki R, Patel S, et al. Genistein encapsulated inulin-stearic acid bioconjugate nanoparticles: Formulation development, characterization and anticancer activity[J]. Int J Biol Macromol, 2022, 206: 213-221.

[37]

Bian Q, Liu J, Tian J, et al. Binding of genistein to human serum albumin demonstrated using tryptophan fluorescence quenching[J]. Int J Biol Macromol, 2004, 34(5): 333-337.

[38]

Abdelwahab HE, Elhag M, El Sadek MM. Removal of As(V) and Cr(VI) using quinoxaline chitosan schiff base: synthesis, characterization and adsorption mechanism[J]. BMC Chem, 2024, 18(1): 225.

[39]

El-Aassar MR, Ibrahim OM, Fouda MMG, et al. Wound dressing of chitosan-based-crosslinked gelatin/ polyvinyl pyrrolidone embedded silver nanoparticles, for targeting multidrug resistance microbes[J]. Carbohydr Polym, 2021, 255: 117484.

[40]

Rosiak N, Tykarska E, Miklaszewski A, et al. Enhancing the Solubility and Dissolution of Apigenin: Solid Dispersions Approach[J]. Int J Mol Sci, 2025, 26(2): 566.

[41]

Su D, Bai M, Wei C, et al. Combining solubilization and controlled release strategies to prepare pH-sensitive solid dispersion loaded with albendazole: in vitro and in vivo studies[J]. Front Vet Sci, 2024, 11: 1522856.

[42]

Rumpf J, Burger R, Schulze M. Statistical evaluation of DPPH, ABTS, FRAP, and Folin-Ciocalteu assays to assess the antioxidant capacity of lignins[J]. Int J Biol Macromol, 2023, 233: 123470.

[43]

Martynek D, Ridvan L, Sivén M, et al. Stability and recrystallization of amorphous solid dispersions prepared by hot-melt extrusion and spray drying[J]. Int J Pharm, 2025, 672: 125331.

[44]

Coelho L, Almeida IF, Sousa Lobo JM, et al. Photostabilization strategies of photosensitive drugs[J]. Int J Pharm, 2018, 541(1-2): 19-25.

[45]

Serajuddin AT. Solid dispersion of poorly water-soluble drugs: early promises, subsequent problems, and recent breakthroughs[J]. J Pharm Sci, 1999, 88(10): 1058-1066.

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