Preparation of Free-Flowing Spray-Dried Amorphous Composites Using Neusilin^®

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Drug Delivery

Background:

• Amorphous solid dispersions (ASDs) aim to enhance the solubility and bioavailability of poorly soluble drugs.
• Processing challenges, such as poor flowability, often hinder the manufacturing of ASDs.
• Neusilin®, a porous additive, is explored for its potential to improve the bulk properties of ASDs.

Purpose of the Study:

• To investigate the impact of Neusilin® on the processability and performance of spray-dried amorphous composite (AC) powders.
• To compare the efficacy of two Neusilin® grades (US2 and UFL2) in enhancing ASD properties.
• To evaluate the dissolution rate and physical stability of drug-loaded AC powders.

Main Methods:

• Spray drying was used to produce amorphous composite (AC) powders with Griseofulvin (GF) and Neusilin®.
• Flowability was assessed using the flow function coefficient (FFC).
• Dissolution studies and 3-month ambient storage stability tests were conducted.

Main Results:

• AC powders with Neusilin® exhibited significantly enhanced flowability (FFC > 10) despite their fine particle size (< 50 μm).
• Griseofulvin (GF) supersaturation up to 3 times crystalline concentration was achieved within 30 minutes, with 80% drug release in 4 minutes.
• Neusilin® addition improved flowability more than in ASDs without the additive, and AC powders maintained amorphous GF state after 3 months.

Conclusions:

• Neusilin® effectively improves the flowability and dissolution rate of spray-dried amorphous composite powders.
• The enhanced properties achieved with Neusilin® can outweigh potential decreases in drug loading.
• This additive offers a promising strategy for overcoming processing challenges in ASD manufacturing.