Aspartame as a co-former in co-amorphous systems

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Drug Delivery

Background:

• Co-amorphous systems improve oral bioavailability of poorly water-soluble drugs.
• Amino acids are known to stabilize amorphous drug forms and enhance dissolution.
• Aspartame, a dipeptide derivative, was explored as a novel co-former.

Purpose of the Study:

• To investigate aspartame's efficacy as a co-former for poorly water-soluble drugs.
• To compare aspartame with single amino acids as co-formers.
• To evaluate the impact on drug dissolution and supersaturation.

Main Methods:

• Ball milling of drug-aspartame mixtures.
• Modulated differential scanning calorimetry (mDSC) for thermal analysis.
• Powder dissolution testing.

Main Results:

• Drug-aspartame mixtures formed amorphous systems, confirmed by a single glass transition temperature (Tg).
• Dissolution rates of mebendazole, tadalafil, and piroxicam were significantly increased from co-amorphous samples.
• Supersaturation was achieved for mebendazole- and tadalafil-aspartame co-amorphous systems.

Conclusions:

• Aspartame is a promising co-former for creating single-phase co-amorphous drug delivery systems.
• Aspartame demonstrated superior performance over single amino acids or their mixtures.
• Co-amorphous systems with aspartame enhance drug dissolution and can induce supersaturation.