Co-crystals of non-steroidal anti-inflammatory drugs (NSAIDs): insight toward formation, methods, and drug enhancement

André L.C.S. Nascimento, Richard P. Fernandes, Maxime D. Charpentier, Joop H. ter Horst, Flávio J. Caires, Marlus Chorilli

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)

Abstract

Pharmaceutical co-crystals have been explored by many researchers as a strategy to optimize physicochemical properties of solid-state drugs. Their improvements of solubility, bioavailability, and the reduced tendency for phase transformation occurrence, are factors that highlight benefits of pharmaceutical co-crystals among other solid forms. According to the Biopharmaceutical Classification System (BCS), non-steroidal anti-inflammatory drugs (NSAIDs) are class II drugs, which have low aqueous solubility and therefore co-crystallization has the potential to optimize NSAID product properties. In this review, we highlight the recent progress made on NSAIDs co-crystals, their co-formers, synthesis, methods and use, while we underline some promising results on in vitro and in vivo co-crystal properties. A celecoxib-tramadol co-crystal reaches phase III clinical trials, showing greater analgesic activity than both individual APIs. The aqueous solubility of the co-crystal formed between L-proline and diclofenac is very high in comparison with the pure drug. Naproxen co-crystals with urea and thiourea have an increase of drug release of almost 60%. Co-crystal design brings a new perspective in drug development since the co-former used can also be a biologically active component allowing to combine different anti-inflammatory drugs, which have an incredible spectrum of application due to the analgesic, anti-pyretic and anti-inflammatory properties.

Original languageEnglish
Pages (from-to)227-241
Number of pages15
JournalParticuology
Volume58
Early online date24 Apr 2021
DOIs
Publication statusE-pub ahead of print - 24 Apr 2021

Keywords

  • bioavailability
  • co-crystal discovery
  • NSAIDs
  • pharmaceutical co-crystals
  • supramolecular synthons

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