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<p> Baicalein, a flavonoid derived from <i>Scutellaria baicalensis</i>, is known for its diverse pharmacological properties, including anti-angiogenic activity. However, its clinical translation is limited due to poor water solubility and low bioavailability. This study aimed to enhance the anti-angiogenic efficacy of baicalein through nanoformulation and evaluate its potential using the <i>in ovo</i> chick chorioallantoic membrane (CAM) assay. Nanoformulated baicalein (NF-b) was prepared via solvent precipitation method using hexane as an anti-solvent and sodium dodecyl sulfate (SDS) as the stabilizer. The formulation was characterized using UV-Vis spectroscopy, dynamic light scattering (DLS), zeta potential analysis, Fourier-transform infrared spectroscopy (FT-IR), and scanning electron microscopy (SEM). Drug release kinetics was studied using the dialysis membrane method. Biocompatibility was assessed via hemolytic assay. Cell viability was assessed using the MTT assay on L929 fibroblast cells. Anti-angiogenic potential of native baicalein and NF-b was evaluated on <i>in ovo</i> CAM assay at 5, 10, and 20µg/mL, and quantified the blood vessels using AngioTool64 software. Mechanistic validation was conducted in CAM model through mRNA expression analysis of VEGF-A, VEGFR-2, and FGF2. NF-b exhibited improved solubility in water and a reduced particle size (~189 nm), with a zeta potential of −43.3 mV indicating good colloidal stability. FT-IR confirmed the retention of key functional groups, while SEM revealed spherical nanoparticles. Hemolytic assay results confirmed biocompatibility at lower doses. MTT results demonstrated dose-dependent cytotoxicity, with significant reductions in viability at higher concentrations (100–200 µg/mL, p &lt; 0.01), and IC₅₀ values of 179.86 µg/mL (native) and 159.60 µg/mL (NF-b). In the CAM assay, NF-b demonstrated a clear dose-dependent inhibition of angiogenesis, with 20 µg/mL reducing vessel area to 0.57-fold, vessel length to 0.58-fold, and junctions to 0.36-fold relative to control (all p &lt; 0.001), surpassing the effect of native baicalein. Mechanistic analysis confirmed significant downregulation of VEGF-A (~0.35-fold), VEGFR-2 (~0.24-fold), and FGF2 (~0.26-fold) in NF-b–treated CAM tissues (p &lt; 0.001). Nanoformulation significantly enhances the solubility, stability, and anti-angiogenic activity of baicalein. The combined CAM inhibition and molecular downregulation of VEGF-A, VEGFR-2, and FGF2 position NF-b as a promising preclinical anti-angiogenic candidate, requiring further endothelial cell-based and in vivo studies for translational progression.</p>

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Anti-Angiogenic Effects of Nanoformulated Baicalein on In Ovo Chick Chorioallantoic Membrane Model: a Physicochemical and Biological Evaluation

  • 期刊论文

  • 发表日期：

    2026年2月25日

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  • Santhosh Kumar Yasam,
  • Antinate Shilpa,
  • Shamini Muthu

摘要

Baicalein, a flavonoid derived from Scutellaria baicalensis, is known for its diverse pharmacological properties, including anti-angiogenic activity. However, its clinical translation is limited due to poor water solubility and low bioavailability. This study aimed to enhance the anti-angiogenic efficacy of baicalein through nanoformulation and evaluate its potential using the in ovo chick chorioallantoic membrane (CAM) assay. Nanoformulated baicalein (NF-b) was prepared via solvent precipitation method using hexane as an anti-solvent and sodium dodecyl sulfate (SDS) as the stabilizer. The formulation was characterized using UV-Vis spectroscopy, dynamic light scattering (DLS), zeta potential analysis, Fourier-transform infrared spectroscopy (FT-IR), and scanning electron microscopy (SEM). Drug release kinetics was studied using the dialysis membrane method. Biocompatibility was assessed via hemolytic assay. Cell viability was assessed using the MTT assay on L929 fibroblast cells. Anti-angiogenic potential of native baicalein and NF-b was evaluated on in ovo CAM assay at 5, 10, and 20µg/mL, and quantified the blood vessels using AngioTool64 software. Mechanistic validation was conducted in CAM model through mRNA expression analysis of VEGF-A, VEGFR-2, and FGF2. NF-b exhibited improved solubility in water and a reduced particle size (~189 nm), with a zeta potential of −43.3 mV indicating good colloidal stability. FT-IR confirmed the retention of key functional groups, while SEM revealed spherical nanoparticles. Hemolytic assay results confirmed biocompatibility at lower doses. MTT results demonstrated dose-dependent cytotoxicity, with significant reductions in viability at higher concentrations (100–200 µg/mL, p < 0.01), and IC₅₀ values of 179.86 µg/mL (native) and 159.60 µg/mL (NF-b). In the CAM assay, NF-b demonstrated a clear dose-dependent inhibition of angiogenesis, with 20 µg/mL reducing vessel area to 0.57-fold, vessel length to 0.58-fold, and junctions to 0.36-fold relative to control (all p < 0.001), surpassing the effect of native baicalein. Mechanistic analysis confirmed significant downregulation of VEGF-A (~0.35-fold), VEGFR-2 (~0.24-fold), and FGF2 (~0.26-fold) in NF-b–treated CAM tissues (p < 0.001). Nanoformulation significantly enhances the solubility, stability, and anti-angiogenic activity of baicalein. The combined CAM inhibition and molecular downregulation of VEGF-A, VEGFR-2, and FGF2 position NF-b as a promising preclinical anti-angiogenic candidate, requiring further endothelial cell-based and in vivo studies for translational progression.