Soluplus-Mediated Diosgenin Amorphous Solid Dispersion with High Solubility and High Stability: Development,...

Area of Science:

• Pharmaceutical Science
• Drug Delivery Systems
• Materials Science

Background:

• Diosgenin (Dio), a traditional Chinese medicine, exhibits anti-tumor, anti-infective, and anti-allergic properties.
• Commercial application of Dio is hindered by its poor aqueous solubility and low bioavailability.
• Soluplus, a novel excipient, offers excellent solubilization and crystallization inhibition capabilities.

Purpose of the Study:

• To develop Soluplus-mediated amorphous solid dispersions (ASDs) of diosgenin (Dio).
• To enhance the solubility, bioavailability, and stability of Dio through ASD formulation.
• To explore the pharmaceutical potential of Dio ASDs.

Main Methods:

• Excipient selection via crystallization inhibition studies (solvent shift method).
• Optimization of ASD preparation methods and drug-excipient ratios based on solubility and dissolution.
• Characterization of Dio-Soluplus interactions using DSC, FT-IR, SEM, PXRD, and molecular docking.
• Evaluation of oral bioavailability through pharmacokinetic studies in rats.
• Assessment of long-term stability of Dio ASDs.

Main Results:

• Soluplus was identified as a suitable excipient for improving Dio solubility and stability.
• Optimized ASDs significantly increased Dio's aqueous solubility via amorphization and molecular interactions.
• Pharmacokinetic studies showed a five-fold improvement in Dio's bioavailability from ASDs.
• Dio ASDs exhibited good stability after storage at 40°C/75% humidity for six months.

Conclusions:

• Soluplus-mediated Dio ASDs offer a promising approach for pharmaceutical applications.
• The developed ASDs demonstrate significantly enhanced solubility, bioavailability, and stability of diosgenin.
• This formulation strategy could overcome the limitations of diosgenin for therapeutic use.