6-Carboxycellulose Acetate Butyrate: Effectiveness as an Amorphous Solid Dispersion Polymer

Area of Science:

• Materials Science
• Pharmaceutical Technology
• Polymer Chemistry

Background:

• Amorphous solid dispersions (ASDs) improve solubility and bioavailability of poorly water-soluble drugs.
• 6-Carboxycellulose acetate butyrate (CCAB) is a novel amphiphilic polymer with a high glass transition temperature, suitable for ASD applications.

Purpose of the Study:

• To evaluate CCAB's potential as a polymer matrix for creating ASDs.
• To assess CCAB's ability to enhance drug solubility and control drug release.

Main Methods:

• Spray drying was used to prepare CCAB/drug amorphous solid dispersions.
• Diverse drugs (quercetin, ibuprofen, ritonavir, loratadine, clarithromycin) were dispersed in CCAB.
• In vitro solubility enhancement and drug release profiles were evaluated.

Main Results:

• CCAB formed amorphous solid dispersions up to 25 wt% drug (loratadine up to 50%).
• Solubility enhancement was observed for quercetin and ritonavir but not for ibuprofen, clarithromycin, or loratadine.
• CCAB provided controlled release of ibuprofen and protected clarithromycin from degradation at stomach pH.

Conclusions:

• CCAB shows promise for creating amorphous solid dispersions, enhancing solubility for certain drugs.
• Its controlled release properties are beneficial for specific drug formulations, like those with stomach irritants.
• Co-polymerization with poly(vinylpyrrolidone) (PVP) further improved CCAB ASD performance.