Design and Evaluation of Novel Solid Self-Nanodispersion Delivery System for Andrographolide

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Nanotechnology

Background:

• Poorly water-soluble drugs present formulation challenges for achieving adequate bioavailability.
• Andrographolide (Andro) is a poorly soluble compound with therapeutic potential.
• Enhancing the dissolution rate is crucial for improving the oral bioavailability of such drugs.

Purpose of the Study:

• To develop a novel solid self-nanodispersion delivery system (Andro-SNDS) for andrographolide (Andro).
• To enhance the dissolution rate and oral bioavailability of Andro using nanocrystal and direct compression technologies.

Main Methods:

• Preparation of Andro nanosuspensions (Andro-NS) via homogenization (approx. 500 nm particle size).
• Conversion of Andro-NS into dried nanocrystal particles (Andro-NP) using spray-drying.
• Fabrication of Andro-SNDS by direct compression of Andro-NP.

Main Results:

• Andro nanocrystals retained their original crystallinity, confirmed by DSC and PXRD.
• The Andro-SNDS formulation exhibited a dissolution rate of 85.87% in pure water within 30 min.
• Significantly higher Cmax (299.32 ng/mL) and AUC0-∞ (4440.55 mg/L·h) for Andro-SNDS compared to crude Andro.
• AUC of Andro-SNDS was 3.09 times higher than that of crude Andro.

Conclusions:

• The developed solid self-nanodispersion delivery system effectively improves the oral bioavailability of andrographolide.
• Combining nanocrystal technology with direct compression offers a promising approach for formulating poorly water-soluble drugs.
• This novel system addresses bioavailability challenges for andrographolide and potentially other similar compounds.