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<p>Baicalein and wogonin, bioactive flavonoids derived from <i>Scutellaria baicalensis</i> Georgi (SBG) via supercritical CO₂ extraction, exhibit potent anti-tumor activity but are hindered by poor solubility and low oral bioavailability. To address these limitations, we developed an optimized self-microemulsifying drug delivery system (SMEDDS) loaded with SBG supercritical extract (SBG-MEs), which demonstrated favorable physicochemical properties, including nanoscale particle size (&lt; 100&#xa0;nm) and high drug loading capacity (5.3%). In vitro, SBG-MEs significantly enhanced cytotoxicity in HepG2 cells, reducing the IC₅₀ from 35.64 ± 1.97&#xa0;µg/mL (crude extract) to 18.74 ± 2.08&#xa0;µg/mL, while cellular uptake increased 2.5-fold, correlating with elevated apoptosis induction. Pharmacokinetic studies in rats demonstrated that SBG-MEs significantly prolonged systemic circulation and achieved higher plasma concentrations of baicalein and wogonin compared to conventional SBG water extracts or supercritical CO₂ extracts. Notably, the AUC<sub>(0−24)</sub> of SBG-MEs was approximately 5.89-fold higher than that of the supercritical CO₂ extract group, indicating enhanced bioavailability. In H22 tumor-bearing mice, SBG-MEs combined with cisplatin achieved superior anti-tumor efficacy (56.83% tumor suppression vs. 33.96% for cisplatin alone) while mitigating cisplatin-induced hepatorenal toxicity and immune organ damage. These findings demonstrate that SMEDDS effectively enhances the oral bioavailability and therapeutic potential of SBG supercritical extract, offering a promising strategy to overcome delivery challenges and potentiate combination therapy in cancer treatment.</p> Graphical abstract <p></p>

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SMEDDS Loaded with Scutellaria baicalensis Georgi Supercritical Extract Enhances Oral Bioavailability and Anti-Tumor Efficacy

  • 期刊论文

  • 发表日期：

    2025年12月17日

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  • Jingqiu Zhang,
  • Ke Wang,
  • Yinxia Chang,
  • Lifen Mu,
  • Yue Zhang,
  • Xuemei Qin

摘要

Baicalein and wogonin, bioactive flavonoids derived from Scutellaria baicalensis Georgi (SBG) via supercritical CO₂ extraction, exhibit potent anti-tumor activity but are hindered by poor solubility and low oral bioavailability. To address these limitations, we developed an optimized self-microemulsifying drug delivery system (SMEDDS) loaded with SBG supercritical extract (SBG-MEs), which demonstrated favorable physicochemical properties, including nanoscale particle size (< 100 nm) and high drug loading capacity (5.3%). In vitro, SBG-MEs significantly enhanced cytotoxicity in HepG2 cells, reducing the IC₅₀ from 35.64 ± 1.97 µg/mL (crude extract) to 18.74 ± 2.08 µg/mL, while cellular uptake increased 2.5-fold, correlating with elevated apoptosis induction. Pharmacokinetic studies in rats demonstrated that SBG-MEs significantly prolonged systemic circulation and achieved higher plasma concentrations of baicalein and wogonin compared to conventional SBG water extracts or supercritical CO₂ extracts. Notably, the AUC(0−24) of SBG-MEs was approximately 5.89-fold higher than that of the supercritical CO₂ extract group, indicating enhanced bioavailability. In H22 tumor-bearing mice, SBG-MEs combined with cisplatin achieved superior anti-tumor efficacy (56.83% tumor suppression vs. 33.96% for cisplatin alone) while mitigating cisplatin-induced hepatorenal toxicity and immune organ damage. These findings demonstrate that SMEDDS effectively enhances the oral bioavailability and therapeutic potential of SBG supercritical extract, offering a promising strategy to overcome delivery challenges and potentiate combination therapy in cancer treatment.

Graphical abstract