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

Autor(es)

Nascimento, Andre L. C. S. ^[1] ; Fernandes, Richard P. ^[2] ; Charpentier, Maxime D. ^[3] ; ter Horst, Joop H. ^[3] ; Caires, Flavio J. ^[4] ; Chorilli, Marlus ^[1]

Afiliação do(s) autor(es)

^[1] Sao Paulo State Univ UNESP, BR-14800903 Araraquara, SP - Brazil

^[2] Sao Paulo State Univ UNESP, Inst Chem, BR-14800060 Araraquara, SP - Brazil

^[3] Univ Strathclyde, EPSRC Ctr Innovat Mfg Continuous Mfg & Crystalli, Glasgow, Lanark - Scotland

^[4] Sao Paulo State Univ UNESP, Sch Sci, BR-17033260 Bauru, SP - Brazil

• Tipo de documento: Artigo de Revisão
• Fonte: PARTICUOLOGY; v. 58, p. 227-241, OCT 2021.
• Citações Web of Science: 1

Resumo

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. (C) 2021 Chinese Society of Particuology and Institute of Process Engineering, Chinese Academy of Sciences. Published by Elsevier B.V. All rights reserved. (AU)

• Processo FAPESP: 13/09022-7 - Estudos termoanalíticos, síntese e caracterização dos co-cristais sólidos de alguns antibióticos (fluoroquinolonas) com alguns co-formadores
• Beneficiário: Massao Ionashiro
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 18/23357-5 - Cocristais multicomponentes de Anti-Inflamatórios Não Esteróides (AINEs) e Inibidores de Bomba de Prótons (IBPs): desenvolvimento, caracterização e avaliação biológica in vitro e in vivo
• Beneficiário: André Luiz Carneiro Soares do Nascimento
• Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado
• Processo FAPESP: 18/24378-6 - Síntese, caracterização e estudo termoanalítico de cocristais de Valsartana, Candesartana Cilexetila e Olmesartana medoxomila
• Beneficiário: Flávio Junior Caires
• Modalidade de apoio: Auxílio à Pesquisa - Regular