Co-crystals of non-steroidal anti-inflammatory drugs (NSAIDs): Insight toward formation, methods, and drug enhancement
dc.contributor.author | Nascimento, André L.C.S. [UNESP] | |
dc.contributor.author | Fernandes, Richard P. [UNESP] | |
dc.contributor.author | Charpentier, Maxime D. | |
dc.contributor.author | ter Horst, Joop H. | |
dc.contributor.author | Caires, Flávio J. [UNESP] | |
dc.contributor.author | Chorilli, Marlus [UNESP] | |
dc.contributor.institution | Universidade Estadual Paulista (Unesp) | |
dc.contributor.institution | University of Strathclyde | |
dc.date.accessioned | 2021-06-25T11:15:20Z | |
dc.date.available | 2021-06-25T11:15:20Z | |
dc.date.issued | 2021-10-01 | |
dc.description.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. | en |
dc.description.affiliation | São Paulo State University (UNESP) School of Pharmaceutical Sciences | |
dc.description.affiliation | São Paulo State University (UNESP) Institute of Chemistry | |
dc.description.affiliation | EPSRC Centre for Innovative Manufacturing in Continuous Manufacturing and Crystallisation University of Strathclyde | |
dc.description.affiliation | São Paulo State University (UNESP) School of Sciences | |
dc.description.affiliationUnesp | São Paulo State University (UNESP) School of Pharmaceutical Sciences | |
dc.description.affiliationUnesp | São Paulo State University (UNESP) Institute of Chemistry | |
dc.description.affiliationUnesp | São Paulo State University (UNESP) School of Sciences | |
dc.description.sponsorship | Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) | |
dc.description.sponsorship | Engineering and Physical Sciences Research Council | |
dc.description.sponsorship | Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) | |
dc.format.extent | 227-241 | |
dc.identifier | http://dx.doi.org/10.1016/j.partic.2021.03.015 | |
dc.identifier.citation | Particuology, v. 58, p. 227-241. | |
dc.identifier.doi | 10.1016/j.partic.2021.03.015 | |
dc.identifier.issn | 2210-4291 | |
dc.identifier.issn | 1674-2001 | |
dc.identifier.scopus | 2-s2.0-85105089298 | |
dc.identifier.uri | http://hdl.handle.net/11449/208635 | |
dc.language.iso | eng | |
dc.relation.ispartof | Particuology | |
dc.source | Scopus | |
dc.subject | Bioavailability | |
dc.subject | Co-crystal discovery | |
dc.subject | NSAIDs | |
dc.subject | Pharmaceutical co-crystals | |
dc.subject | Supramolecular synthons | |
dc.title | Co-crystals of non-steroidal anti-inflammatory drugs (NSAIDs): Insight toward formation, methods, and drug enhancement | en |
dc.type | Artigo |