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<p>Quercetagetin (QTGN), a natural flavonoid with PIM-1 inhibitory effects, can play a vital role in prostate cancer therapy. However, QTGN displays poor water solubility, and in turn, low bioavailability poses challenges for its clinical use. In this work, folate receptor-targeted quercetagetin-loaded mixed micelles (Q-MMs) were prepared by the solvent evaporation method using folic acid-conjugated pluronic F-127 and Soluplus and optimized using a 3<sup>2</sup> factorial design. Q-MMs were characterized for size, entrapment efficiency, FTIR, DSC, PXRD, TEM, in vitro drug release, cytotoxicity evaluation and apoptosis analysis in human prostate cancer (PC-3) cells and in vivo pharmacokinetics in rats. Q-MMs displayed near-spherical morphology with PS of 41.6 ± 2.1&#xa0;nm, a zeta potential of -23 ± 0.6 mV, and an entrapment efficiency of 86 ± 2.7%. Q-MMs displayed pH-dependent sustained QTGN release following Higuchi model. Q-MMs exhibited IC<sub>50</sub> of 24.22 ± 2.3 µM with 2.1-fold greater apoptosis induction in PC-3 cells when compared to QTGN alone. Further pharmacokinetic data of Q-MMs suggested 2.13 and 7-fold increase in AUC<sub>₀–t</sub> and C<sub>max,</sub> respectively, when compared with QTGN alone. Thus, the present work reports Q-MMs nanomicelles as a promising therapeutic strategy for the treatment of prostate cancer.</p> Graphical Abstract <p></p>

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Formulation and Characterization of Folate Receptor-Targeted Quercetagetin-Loaded Mixed Micelles With Enhanced Oral Bioavailability and Anticancer Efficacy Against Human Prostate Cancer Cells

  • 期刊论文

  • 发表日期：

    2026年1月16日

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  • Smita Suryawanshi,
  • Sharvil Patil

摘要

Quercetagetin (QTGN), a natural flavonoid with PIM-1 inhibitory effects, can play a vital role in prostate cancer therapy. However, QTGN displays poor water solubility, and in turn, low bioavailability poses challenges for its clinical use. In this work, folate receptor-targeted quercetagetin-loaded mixed micelles (Q-MMs) were prepared by the solvent evaporation method using folic acid-conjugated pluronic F-127 and Soluplus and optimized using a 32 factorial design. Q-MMs were characterized for size, entrapment efficiency, FTIR, DSC, PXRD, TEM, in vitro drug release, cytotoxicity evaluation and apoptosis analysis in human prostate cancer (PC-3) cells and in vivo pharmacokinetics in rats. Q-MMs displayed near-spherical morphology with PS of 41.6 ± 2.1 nm, a zeta potential of -23 ± 0.6 mV, and an entrapment efficiency of 86 ± 2.7%. Q-MMs displayed pH-dependent sustained QTGN release following Higuchi model. Q-MMs exhibited IC50 of 24.22 ± 2.3 µM with 2.1-fold greater apoptosis induction in PC-3 cells when compared to QTGN alone. Further pharmacokinetic data of Q-MMs suggested 2.13 and 7-fold increase in AUC₀–t and Cmax, respectively, when compared with QTGN alone. Thus, the present work reports Q-MMs nanomicelles as a promising therapeutic strategy for the treatment of prostate cancer.

Graphical Abstract