Pharmaceutical cocrystals, salts and multicomponent systems; intermolecular interactions and property based design

Area of Science:

• Pharmaceutical Science
• Materials Science
• Drug Development

Background:

• Small molecule drug development faces increasing challenges in cost-effectiveness and efficiency.
• Improving the physical properties of Active Pharmaceutical Ingredients (APIs) without altering covalent chemistry is crucial for global health.
• Multicomponent solid forms, including pharmaceutical salts, cocrystals, and coamorphous systems, offer strategies for API property enhancement.

Purpose of the Study:

• To review current strategies and state-of-the-art approaches in pharmaceutical multicomponent phase design.
• To discuss the role of intermolecular interactions in the formation and properties of these phases.
• To highlight the implications of these interactions on material properties and patient pharmacokinetics.

Main Methods:

• Review of existing literature on pharmaceutical salts, cocrystals, and coamorphous systems.
• Analysis of intermolecular interactions governing multicomponent solid formation.
• Evaluation of the impact of these interactions on physical properties and pharmacokinetic profiles.

Main Results:

• Pharmaceutical salts, cocrystals, and coamorphous systems represent established and emerging methods for API property modulation.
• Understanding and controlling intermolecular interactions are key to rationally designing effective multicomponent phases.
• These interactions significantly influence material properties (e.g., solubility, stability) and in-vivo performance.

Conclusions:

• Multicomponent solid-state engineering is a critical strategy for overcoming challenges in small molecule drug development.
• Rational design based on intermolecular interactions enables optimization of API properties for improved therapeutic outcomes.
• Further research into the predictive power of interaction analysis will advance the development of advanced drug delivery systems.