Drug Delivery through Co-amorphous Solid Dispersions: A Comprehensive and Updated Review on Physicochemical...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery
• Materials Science

Background:

• Poor aqueous solubility and permeability of new chemical entities pose significant formulation challenges.
• Low solubility leads to slow dissolution, poor bioavailability, and unpredictable toxicity.
• Enhancing solubility, dissolution, and bioavailability is crucial for drug development.

Purpose of the Study:

• To review challenges, improvements, and innovations in co-amorphous systems for drug formulation.
• To provide a comprehensive explanation of established and emerging methods for characterizing co-amorphous solid dispersions (CASD).
• To highlight the potential of CASD in improving patient outcomes and therapeutic efficacy.

Main Methods:

• Coamorphization strategy utilizing co-amorphous solid dispersions (CASD).
• Evaluation of co-former selection and surface properties of co-amorphous formulations.
• In vitro and in vivo characterization of physicochemical attributes and biological performance of CASD.

Main Results:

• Coamorphization enhances solubility and amorphous stability of BCS Class II medications.
• CASD, comprising drug(s) and co-former(s), improves drug bioavailability and physical stability.
• Careful evaluation of co-former properties and formulation surface characteristics is critical for stability and performance.

Conclusions:

• Co-amorphous solid dispersions (CASD) represent a promising strategy for overcoming solubility and bioavailability challenges.
• CASD offer improved physical stability and therapeutic efficacy for challenging drug candidates.
• Addressing scale-up and processing challenges is essential for the clinical application of CASD.