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Etidronate-based organic salts and ionic liquids: In vitro effects on bone metabolism

2021-12-15Journal article Restricted access
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dc.contributor.authorTeixeira, Sónia
dc.contributor.authorSantos, Miguel M.
dc.contributor.authorBranco, Luís C.
dc.contributor.authorCosta-Rodrigues, João
dc.date.accessioned2022-02-15T12:04:05Z
dc.date.available2022-02-15T12:04:05Z
dc.date.issued2021-12-15
dc.description.abstractBisphosphonates are a class of drugs widely used for the treatment of several pathologies associated with increased bone resorption. Although displaying low oral bioavailability, these drugs have the ability to accumulate in bone matrix, where the biological effects are exerted. In the present work, four mono- and dianionic Etidronate-based Organic Salts and Ionic Liquids (Eti-OSILs) were developed by combination of this drug with the superbases 1,1,3,3-tetramethylguanidine (TMG) and 1,5-diazabicyclo(4.3.0)non-5-ene (DBN) as cations, aiming to improve not only the physicochemical properties of this seminal bisphosphonate, but also its efficacy in the modulation of cellular behavior, particularly on human osteoclasts and osteoblasts. It was observed that some of the developed compounds, in particular the dianionic ones, presented very high water solubility and diminished or absent polymorphism. Also, several of them appeared to be more cytotoxic against human breast and osteosarcoma cancer cell lines while retaining low toxicity to normal cells. Regarding bone cells, a promotion of an anabolic state was observed for all Eti-OSILs, primarily for the dianionic ones, which leads to an inhibition of osteoclastogenesis and an increase in osteoblastogenesis. The observed effects resulted from differential modulation of intracellular signaling pathways by the Eti-OSILs in comparison with Etidronate. Hence, these results pave the way for the development of more efficient and bioavailable ionic formulations of bisphosphonates aiming to effectively modulate bone metabolism, particularly in the case of increased bone resorption.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationTeixeira, S., Santos, M. M., Branco, L. C., & Costa-Rodrigues, J. (2021). Etidronate-based organic salts and ionic liquids: In vitro effects on bone metabolism. International Journal of Pharmaceutics, 610, 121262. https://doi.org/https://doi.org/10.1016/j.ijpharm.2021.121262pt_PT
dc.identifier.doi10.1016/j.ijpharm.2021.121262pt_PT
dc.identifier.eissn1873-3476
dc.identifier.urihttp://hdl.handle.net/10400.22/19979
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherElsevierpt_PT
dc.relation.publisherversionhttps://www.sciencedirect.com/science/article/pii/S0378517321010681?via%3Dihub#kg005pt_PT
dc.subjectBisphosphonatespt_PT
dc.subjectEtidronateIonic liquidspt_PT
dc.subjectOsteoclastogenesispt_PT
dc.titleEtidronate-based organic salts and ionic liquids: In vitro effects on bone metabolismpt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.citation.endPage12pt_PT
oaire.citation.startPage1pt_PT
oaire.citation.titleInternational Journal of Pharmaceuticspt_PT
oaire.citation.volume610pt_PT
person.familyNameCosta-Rodrigues
person.givenNameJoao
person.identifier.ciencia-id7412-B006-2120
person.identifier.orcid0000-0003-1375-8067
person.identifier.scopus-author-id8558383400
rcaap.rightsclosedAccesspt_PT
rcaap.typearticlept_PT
relation.isAuthorOfPublicationce85cc8f-09f3-4c26-aeaf-6128971acf68
relation.isAuthorOfPublication.latestForDiscoveryce85cc8f-09f3-4c26-aeaf-6128971acf68

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