ArticleAAPS PharmSciTech2025
Novel Quercetin-Ascorbic Acid Nano Cocrystals: A Carrier-free Strategy for Enhancement of Solubility, Topical Anti-oxidant Activity and Cytotoxicity.
Article in AAPS PharmSciTech, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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7 authors.
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Abstract
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.
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