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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

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

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Author(s):
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]
Total Authors: 6
Affiliation:
[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
Total Affiliations: 4
Document type: Review article
Source: PARTICUOLOGY; v. 58, p. 227-241, OCT 2021.
Web of Science Citations: 1
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. (C) 2021 Chinese Society of Particuology and Institute of Process Engineering, Chinese Academy of Sciences. Published by Elsevier B.V. All rights reserved. (AU)

FAPESP's process: 13/09022-7 - Thermoanalytical studies, synthesis and characterization of the solid co-crystals of antibiotics (fluoroquinolones) with some co-formers
Grantee:Massao Ionashiro
Support Opportunities: Regular Research Grants
FAPESP's process: 18/23357-5 - Multidrug co-crystals of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) and Proton Pump Inhibitors (PPIs): development, characterization and biological evaluation in vitro and in vivo
Grantee:André Luiz Carneiro Soares do Nascimento
Support Opportunities: Scholarships in Brazil - Post-Doctoral
FAPESP's process: 18/24378-6 - Synthesis, characterization and thermoanalytical study of Valsartan, Candesartan Cilexetil and Olmesartan medoxomil co-crystals
Grantee:Flávio Junior Caires
Support Opportunities: Regular Research Grants