Development of fast-dissolving dosage forms of curcuminoids by electrospinning for potential tumor therapy application

Abstract

Curcuminoids (CUs) of antitumor and various other potential biological activities have extremely low water solubility therefore special formulation was elaborated. New fast dissolving reconstitution dosage forms of four CUs were prepared as fibrous form of 2-hydroxypropyl-β-cyclodextin (HP-β-CD). In the electrospinning process HP-β-CD could act both as solubilizer and fiber-forming agent. The solubilization efficiency of the CU-HP-β-CD systems was determined with phase-solubility measurements. The electrospun CUs were amorphous and uniformly distributed in the fibers according to XRD analysis and Raman mappings. The fibrous final products had fast (<5 min) and complete dissolution. In typical iv. infusion reconstitution volume (20 mL) fibers containing 40-80 mg of CU could be dissolved, which is similar to the currently proposed dose (<120 mg/m²). The in vitro cytostatic effect data showed that the antitumor activity of the CU-HP-β-CD complexes was similar or better compared to the free APIs.

Keywords: Aqueous electrospinning; Curcumin; Curcuminoids; Cyclodextrin; Fast-dissolving.