Rubusoside As a Multifunctional Stabilizer for Novel Nanocrystal-Based Solid Dispersions with a High Drug Loading: A...

Area of Science:

• Pharmaceutical Science
• Materials Science
• Drug Delivery

Background:

• Poorly soluble drugs present significant challenges in oral bioavailability.
• Nanocrystal and solid dispersion technologies are key strategies to enhance drug solubility and delivery.

Purpose of the Study:

• To develop novel nanocrystalline solid dispersions (NCSDs) for improved oral delivery of insoluble drugs.
• To utilize rubusoside as a multifunctional stabilizer for apigenin nanocrystal-based solid dispersions (AP-NSD).

Main Methods:

• Preparation of AP-NSD using homogenization and spray-drying technologies.
• Characterization of AP-NSD using IR, SEM, TEM, DSC, and PXRD.
• Assessment of in vitro dissolution rates compared to API and amorphous solid dispersions (AP-ASD).

Main Results:

• Rubusoside (20%) stabilized AP-NSD demonstrated high drug-loading, good redispersibility, and enhanced stability.
• AP-NSD exhibited a significantly higher in vitro dissolution rate compared to apigenin API and AP-ASD.
• The improved dissolution may be attributed to the presence of rubusoside on the drug's surface.

Conclusions:

• The developed AP-NSD offers a promising and effective approach for the oral delivery of insoluble drugs.
• Rubusoside serves as a natural and safe stabilizer, enhancing the performance of nanocrystalline solid dispersions.
• This technology provides a viable pathway for formulating insoluble Chinese medicine ingredients.