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<p>Quercetin (QUC), an extensively investigated nutraceutical, demonstrates various clinical and therapeutic effects such as anti-oxidant, anti-inflammatory, anti-malarial, anti-viral, anti-carcinogenic and cytoprotective properties. However, the effectiveness of QUC is off-set by its poor solubility, stability, permeability, and absorption. In current research, a cocrystal nanonization strategy, integrating the cocrystallization and nanosizing techniques, has been tested to address intrinsic issues of QUC. A cocrystal of QUC with ascorbic acid (as co-former) synthesized by solvent evaporation was transformed into nano-cocrystal (NCC) by top-down homogenization technique using 0.045% Poloxamer 188 (as stabilizer). NCC was characterized by SEM and Zetasizer and appeared to be blocked-shaped with mean particle size of 300 ± 80&#xa0;nm. Further characterization was undertaken using powder X-ray diffraction, differential scanning calorimetry and Fourier transform infrared spectroscopy. The properties of cocrystal and NCC were explored by solubility, <i>In-vitro</i> dissolution, anti-oxidant, and cytotoxicity studies against Vero and MCF-7 cells. NCC presented 17 and 5 times enhanced solubility and dissolution of QUC in distilled water and 1.6 times enhanced anti-oxidant activity compared to free QUC, and substantial mortality against MCF-7 cells. NCC remained stable in gel for six months at 4 ± 2ºC and 30 ± 2ºC/60 ± 5%RH. The gel released 98.91% QUC after 5&#xa0;h. Hence, the topical formulation by combining the advantages of cocrystals and nanonization (nano-cocrystals) might be a promising strategy in treating various skin ailments by virtue of ameliorated physicochemical profile, anti-oxidant activity and stability.</p> Graphical Abstract <p></p>

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Novel Quercetin-Ascorbic Acid Nano Cocrystals: A Carrier-free Strategy for Enhancement of Solubility, Topical Anti-oxidant Activity and Cytotoxicity

  • 期刊论文

  • 发表日期：

    2025年10月24日

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  • Najam ul Hassan Jawa,
  • Nasir Abbas,
  • Hafiza Nasreen Aslam,
  • Hafsa Afzal,
  • Misbah Hameed,
  • Nadeem Irfan Bukhari,
  • Sumera Latif

摘要

Quercetin (QUC), an extensively investigated nutraceutical, demonstrates various clinical and therapeutic effects such as anti-oxidant, anti-inflammatory, anti-malarial, anti-viral, anti-carcinogenic and cytoprotective properties. However, the effectiveness of QUC is off-set by its poor solubility, stability, permeability, and absorption. In current research, a cocrystal nanonization strategy, integrating the cocrystallization and nanosizing techniques, has been tested to address intrinsic issues of QUC. A cocrystal of QUC with ascorbic acid (as co-former) synthesized by solvent evaporation was transformed into nano-cocrystal (NCC) by top-down homogenization technique using 0.045% Poloxamer 188 (as stabilizer). NCC was characterized by SEM and Zetasizer and appeared to be blocked-shaped with mean particle size of 300 ± 80 nm. Further characterization was undertaken using powder X-ray diffraction, differential scanning calorimetry and Fourier transform infrared spectroscopy. The properties of cocrystal and NCC were explored by solubility, In-vitro dissolution, anti-oxidant, and cytotoxicity studies against Vero and MCF-7 cells. NCC presented 17 and 5 times enhanced solubility and dissolution of QUC in distilled water and 1.6 times enhanced anti-oxidant activity compared to free QUC, and substantial mortality against MCF-7 cells. NCC remained stable in gel for six months at 4 ± 2ºC and 30 ± 2ºC/60 ± 5%RH. The gel released 98.91% QUC after 5 h. Hence, the topical formulation by combining the advantages of cocrystals and nanonization (nano-cocrystals) might be a promising strategy in treating various skin ailments by virtue of ameliorated physicochemical profile, anti-oxidant activity and stability.

Graphical Abstract