Formulation of Curcumin-β-cyclodextrin-polyvinylpyrrolidone supramolecular inclusion complex: experimental, molecular docking, and preclinical anti-inflammatory assessment

Abstract

This research planned to ameliorate an aqueous solubility and dissolution of Curcumin (CUR) by the formulation of inclusion complex with β-cyclodextrin (β-CD) and polyvinylpyrrolidone (PVP). The phase solubility study was performed to assess the solubility of CUR. The prepared CUR complex assessed for dissolution study, physicochemical evaluation, in-vitro antioxidant activity, molecular modeling, and anti-inflammatory assessment. The pivotal findings of phase-solubility studies demonstrate apparent stability constant (Kc) and complexation efficiency (CE) values for CUR-β-CD and CUR-β-CD-PVP complex was 175.4 M⁻¹, 1.15% and 833.3.2 M⁻¹ and 5.21%, respectively. The characterization results revealed amorphization of crystalline state (CUR) into amorphous state. The maximum drug release found with the ternary CUR complex (F7), i.e. 45.41 ± 3.78% in 6 h study. The chemical shift in the NMR supports that the aromatic ring of CUR is completely complexed inside the β-CD cavity. The antioxidant activity of pure CUR was found to be 58.02 ± 2.21% and CUR ternary complex (F7) showed significantly higher activity to 96.02 ± 2.46%. The in-vivo effect of CUR complex (F7) was also found significantly higher than that of pure CUR. The molecular modeling study depicted that PVP increased the stability of the ternary complex by forming the link between CUR and β-CD. Thus, the ternary inclusion complex of CUR-β-CD-PVP could contribute as an innovative outcome in the enhancement of solubility and in-vivo activity.

Keywords:

• Curcumin
• solubility
• inclusion complex
• in-vivo activity
• molecular modeling

Disclosure statement

No potential conflict of interest was reported by the author(s).