Solid state characterization of progesterone in a freeze dried 1:2 progesterone/HPBCD mixture

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Physical Chemistry

Background:

• Progesterone, a vital hormone, exhibits poor aqueous solubility, limiting its therapeutic applications.
• Cyclodextrins, particularly hydroxypropyl-beta-cyclodextrin (HPBCD), are widely used to enhance the solubility of poorly soluble drugs.

Purpose of the Study:

• To investigate the formation and characterization of a progesterone-hydroxypropyl-beta-cyclodextrin (HPBCD) inclusion complex in an aqueous solution.
• To confirm the existence and structure of the inclusion complex in the solid state.

Main Methods:

• Solubilization of progesterone in an aqueous solution with HPBCD at a 1:2 molar ratio.
• Filtration and freeze-drying of the resulting solution to obtain the solid complex.
• Solid-state characterization using Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA), X-ray Diffraction (XRD), Raman spectroscopy, and Fourier-Transform Infrared (FTIR) spectroscopy.

Main Results:

• Progesterone rapidly formed a soluble inclusion complex with HPBCD in aqueous solution.
• Characterization techniques confirmed the formation of the progesterone-HPBCD inclusion complex in the solid state.
• Analysis provided preliminary data on the possible structure of the solid-state inclusion complex.

Conclusions:

• A stable and soluble inclusion complex of progesterone with HPBCD can be successfully prepared.
• Solid-state characterization validates the formation of the inclusion complex, offering potential for improved progesterone formulations.