Co-amorphous systems for the delivery of poorly water-soluble drugs: recent advances and an update

ABSTRACT

Introduction

Most new drug candidates under development are poorly water-soluble, which are related to multiple pharmaceutical issues, increasing the bioavailability of these drugs by the improvement of solubility/dissolution has become a major concern to develop efficacious drugs with reasonable dosing regimens for patients. Over the past decade, increasing reports have been published on the investigation of co-amorphous drug delivery systems, with positive and excited outcomes in improving in vitro and in vivo performances of poorly water-soluble drugs.

Areas covered

This review summarizes recent findings of co-amorphous systems and provides their updates as a comprehensive overview in terms of classification, co-formers selection, preparation methods, physicochemical characteristics and in vivo performances.

Expert opinion

Co-amorphous system, a homogeneous single-phase system containing two compatible drugs or a drug with a pharmaceutically acceptable small-molecule co-former, has been employed as a promising formulation technology to improve in vitro and in vivo performances of poorly water-soluble drugs such as solubility/dissolution, stability, mechanical properties and bioavailability. Furthermore, a deeper understanding of co-amorphous systems, including its detailed classification, the criteria of co-former selection, stability mechanisms and the faced challenges as well as perspectives, will be more conducive to its development and application.

KEYWORDS:

• Co-amorphous
• classification
• co-formers selection
• preparation
• physicochemical characteristics
• bioavailability

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This research was supported by National Natural Science Foundation of China [81703712, 81773675, 81873012], ‘Double First-Class’ University Project (CPU2018GY11, CPU2018GY27), Jiangsu Province Double Innovation Talent Program (2015), Postgraduate Research & Practice Innovation Program of Jiangsu Province.