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Purpose <p>Curcumin (CUM) is a promising nutraceutical and exhibits diverse pharmacological activities such as antioxidant, anti-inflammatory, antitumor and anti-hyperglycemic, but the clinical applications of CUM is restricted by virtue of its scarce aqueous solubility, poor stability and, low oral and topical absorption. In this work a nano-cocrystal strategy, integrating the benefits of cocrystallization and nanocrystal techniques, has been proposed to assess the potential of nano-sized cocrystals as a new insight to address the intrinsic issues of CUM in advance of only cocrystallization or nanonization.</p> Methods <p>A cocrystals (CC) of CUM was successfully synthesized with ascorbic acid by solvent evaporation and then transformed into nano-cocrystal (NCC) by a top down homogenization technique using poloxamer 188 (0.04%w/w) as stabilizer. NCC was characterized through SEM, Zetasizer, DSC, FTIR, PXRD, solubility study, antioxidant activity and cytotoxicity against MCF-7 cells. A topical gel formulation of NCC was developed and underwent stability studies.</p> Results <p>NCC was changed into amorphous state with mean particle size of 200 ± 30&#xa0;nm and presented 16 and 10 fold enhanced solubility (15611 <i>±</i> 0.551&#xa0;µg/mL) and dissolution (91.933 <i>±</i> 0.024%) of CUM in distilled water in comparison to pure CUM solubility (940 <i>±</i> 0.024&#xa0;µg/mL) and percent dissolved (8.467 <i>±</i> 0.304%). NCC displayed 1.5 fold enhanced antioxidant activity (99.154 ± 0.58%) than CUM (65.688 ± 0.02%) with IC<sub>50</sub> value of 1.4 ± 0.180&#xa0;µg/ml and also led to a significant reduction ((<i>p</i> &lt; 0.001) in the viability of MCF-7 breast cancer cells. Additionally, no notable changes were detected in NCC gel at 4 ± 2&#xa0;°C and 30 ± 2&#xa0;°C /65 ± 5% RH during 6 months stability study. In-vitro release studies of NCC gel by modified Franz diffusion cell demonstrated a 2.4fold cumulative release of CUM compared to pure CUM gel. Release data was best fitted to Hixon-Crowell kinetic model with n value (0.695) showing non-fickian release.</p> Conclusion <p>Curcumin-Ascorbic acid NCC showed better solubility, in-vitro dissolution, anti-oxidant and cytotoxic activities, and can be employed in topical gel formulation with utility in various skin ailments.</p>

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Nano-cocrystal Delivery System of Curcumin: Physicochemical Characterization, Antioxidant Activity, Cytotoxicity Against MCF-7 Cells and Topical Gel Formulation

  • 期刊论文

  • 发表日期：

    2026年2月21日

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  • Amna saleem,
  • Hafsa Afzal,
  • Najam ul Hassan jawa,
  • Sairah Hafeez Kamran,
  • Qazi Amir Ijaz,
  • Nasir Abbas,
  • Sumera Latif

摘要

Purpose

Curcumin (CUM) is a promising nutraceutical and exhibits diverse pharmacological activities such as antioxidant, anti-inflammatory, antitumor and anti-hyperglycemic, but the clinical applications of CUM is restricted by virtue of its scarce aqueous solubility, poor stability and, low oral and topical absorption. In this work a nano-cocrystal strategy, integrating the benefits of cocrystallization and nanocrystal techniques, has been proposed to assess the potential of nano-sized cocrystals as a new insight to address the intrinsic issues of CUM in advance of only cocrystallization or nanonization.

Methods

A cocrystals (CC) of CUM was successfully synthesized with ascorbic acid by solvent evaporation and then transformed into nano-cocrystal (NCC) by a top down homogenization technique using poloxamer 188 (0.04%w/w) as stabilizer. NCC was characterized through SEM, Zetasizer, DSC, FTIR, PXRD, solubility study, antioxidant activity and cytotoxicity against MCF-7 cells. A topical gel formulation of NCC was developed and underwent stability studies.

Results

NCC was changed into amorphous state with mean particle size of 200 ± 30 nm and presented 16 and 10 fold enhanced solubility (15611 ± 0.551 µg/mL) and dissolution (91.933 ± 0.024%) of CUM in distilled water in comparison to pure CUM solubility (940 ± 0.024 µg/mL) and percent dissolved (8.467 ± 0.304%). NCC displayed 1.5 fold enhanced antioxidant activity (99.154 ± 0.58%) than CUM (65.688 ± 0.02%) with IC50 value of 1.4 ± 0.180 µg/ml and also led to a significant reduction ((p < 0.001) in the viability of MCF-7 breast cancer cells. Additionally, no notable changes were detected in NCC gel at 4 ± 2 °C and 30 ± 2 °C /65 ± 5% RH during 6 months stability study. In-vitro release studies of NCC gel by modified Franz diffusion cell demonstrated a 2.4fold cumulative release of CUM compared to pure CUM gel. Release data was best fitted to Hixon-Crowell kinetic model with n value (0.695) showing non-fickian release.

Conclusion

Curcumin-Ascorbic acid NCC showed better solubility, in-vitro dissolution, anti-oxidant and cytotoxic activities, and can be employed in topical gel formulation with utility in various skin ailments.