Optimization and in vitro Release Evaluation of Parthenolide-Loaded Neutral γ-CD-MOF Assisted with ScCO₂ Fluid

  OBJECTIVES  Cyclodextrin metal-organic framework (γ-CD-MOF) formed self-assembly by K⁺ions and γ-cyclodextrin (γ-CD) was used as the carrier of PTL in order to improve its solubility and stability.

  METHODS  γ-CD-MOF was prepared by solvothermal method. Neu-γ-CD-MOF was obtained by neutralization and then activated by supercritical carbon dioxide fluid (scCO₂). The preparation of PTL-loaded Neu-γ-CD-MOF assisted with scCO₂ method was optimized, and the PTL@Neu-γ-CD-MOF was systematically characterized and evaluated for release in vitro.

  RESULTS  Neu-γ-CD-MOF with nanoscale particle size and uniform dispersion is obtained after scCO₂ activation. Drug loading of PTL@Neu-γ-CD-MOF is 26.58% assisted with scCO₂. PTL@Neu-γ-CD-MOF significantly increases the water solubility of PTL, and the apparent solubility of PTL in water is 2.2 times of free PTL. The dissolution rate and cumulative release of PTL are both significantly improved.

  CONCLUSION  ScCO₂ can improve drug loading efficiency of Neu-γ-CD-MOF, and PTL@Neu-γ-CD-MOF increases the solubility and dissolution rate of PTL effectively.