<p>Curcumin (CUR) is a polyphenol known for its therapeutic potential, but faces limitations in clinical application due to its poor aqueous solubility and low bioavailability. This study envisaged developing stable ternary inclusion complexes of CUR with β-cyclodextrin (βCD) and ascorbic acid (AA) as the ternary substance. Inclusion complexes were prepared by kneading and autoclaving method. Phase solubility studies revealed that the A<sub>L</sub> type relation between CUR and βCD. We observed The AA improved the stability of the ternary complexes with its stability constant as 138.8M<sup>− 1</sup>, complexation efficiency as 0.198, utility number as 3.96 and the bulk as 4.80. The solubilization power improved from − 17.42 to 1.33. Cytotoxicity assays using the A549 lung cancer cell line demonstrated that the ternary complex exhibits potent anticancer activity, comparable to pure CUR. In vitro dissolution tests showed a marked increase in the release rate of CUR from the ternary complex. Our study demonstrates that the inclusion of AA significantly enhances the solubility, stability, and biological efficacy of CUR. The higher stability constant and complexation efficiency of CUR-βCD-AA was due to improved interaction facilitated by AA. The inclusion complexes showed improved antibacterial activity against <i>Staphylococcus aureas</i> and <i>Staphylococcus epidermis</i> Enhanced dissolution rates and strong cytotoxic effects against A549 lung cancer cells further support the potential of this ternary complex in overcoming CUR’s bioavailability limitations. These results suggest that the CUR-βCD-AA ternary complex effectively enhances curcumin’s solubility, stability, and anticancer activity, offering a promising formulation strategy to overcome curcumin’s bioavailability challenges and improve its therapeutic potential.</p>

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A stable curcumin/β-cyclodextrin/ascorbic acid ternary inclusion complexes, docking studies, antimicrobial and anticancer assays

  • Md Sajid Ali,
  • Nur Sarah binti Zainal Shahrom,
  • Thevashree Rajanderan,
  • Ahmad Salawi,
  • Fahad Y. Sabei,
  • Ahmed H. Albariqi,
  • Muhammad Hadi Sultan,
  • Mohammad Intakhab Alam,
  • Ayed A. Alshamrani,
  • Arun Kumar,
  • Lee Rhi Zhou,
  • Shahnaz Majeed,
  • Mohammed Tahir Ansari

摘要

Curcumin (CUR) is a polyphenol known for its therapeutic potential, but faces limitations in clinical application due to its poor aqueous solubility and low bioavailability. This study envisaged developing stable ternary inclusion complexes of CUR with β-cyclodextrin (βCD) and ascorbic acid (AA) as the ternary substance. Inclusion complexes were prepared by kneading and autoclaving method. Phase solubility studies revealed that the AL type relation between CUR and βCD. We observed The AA improved the stability of the ternary complexes with its stability constant as 138.8M− 1, complexation efficiency as 0.198, utility number as 3.96 and the bulk as 4.80. The solubilization power improved from − 17.42 to 1.33. Cytotoxicity assays using the A549 lung cancer cell line demonstrated that the ternary complex exhibits potent anticancer activity, comparable to pure CUR. In vitro dissolution tests showed a marked increase in the release rate of CUR from the ternary complex. Our study demonstrates that the inclusion of AA significantly enhances the solubility, stability, and biological efficacy of CUR. The higher stability constant and complexation efficiency of CUR-βCD-AA was due to improved interaction facilitated by AA. The inclusion complexes showed improved antibacterial activity against Staphylococcus aureas and Staphylococcus epidermis Enhanced dissolution rates and strong cytotoxic effects against A549 lung cancer cells further support the potential of this ternary complex in overcoming CUR’s bioavailability limitations. These results suggest that the CUR-βCD-AA ternary complex effectively enhances curcumin’s solubility, stability, and anticancer activity, offering a promising formulation strategy to overcome curcumin’s bioavailability challenges and improve its therapeutic potential.