Lipid Formulations and Bioconjugation Strategies for Indomethacin Therapeutic Advances

Indomethacin (IND) is a drug which after successful clinical trials became available for general prescription in 1965 and from that time is one of the most widely used anti-inflammatory drug with the highest potencies in the in vitro and in vivo models. However, despite its high therapeutic efficacy...

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Main Authors: Anna Gliszczyńska, Marta Nowaczyk
Format: Article
Language:English
Published: MDPI AG 2021-03-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/26/6/1576
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author Anna Gliszczyńska
Marta Nowaczyk
author_facet Anna Gliszczyńska
Marta Nowaczyk
author_sort Anna Gliszczyńska
collection DOAJ
description Indomethacin (IND) is a drug which after successful clinical trials became available for general prescription in 1965 and from that time is one of the most widely used anti-inflammatory drug with the highest potencies in the in vitro and in vivo models. However, despite its high therapeutic efficacy in relieving the symptoms of certain arthritis and in treating gout or collagen diseases, administration of IND causes a number of adverse effects, such as gastrointestinal ulceration, frequent central nervous system disorders and renal toxicity. These obstacles significantly limit the practical applications of IND and make that 10–20% of patients discontinue its use. Therefore, during the last three decades many attempts have been made to design novel formulations of IND aimed to increase its therapeutic benefits minimizing its adverse effects. In this review we summarize pharmacological information about IND and analyze its new lipid formulations and lipid bioconjugates as well as discuss their efficacy and potential application.
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spelling doaj.art-b5dde11f244e491991c409bf22d687fa2023-11-21T10:18:45ZengMDPI AGMolecules1420-30492021-03-01266157610.3390/molecules26061576Lipid Formulations and Bioconjugation Strategies for Indomethacin Therapeutic AdvancesAnna Gliszczyńska0Marta Nowaczyk1Department of Chemistry, Wrocław University of Environmental and Life Sciences, Norwida 25, 50-375 Wrocław, PolandDepartment of Chemistry, Wrocław University of Environmental and Life Sciences, Norwida 25, 50-375 Wrocław, PolandIndomethacin (IND) is a drug which after successful clinical trials became available for general prescription in 1965 and from that time is one of the most widely used anti-inflammatory drug with the highest potencies in the in vitro and in vivo models. However, despite its high therapeutic efficacy in relieving the symptoms of certain arthritis and in treating gout or collagen diseases, administration of IND causes a number of adverse effects, such as gastrointestinal ulceration, frequent central nervous system disorders and renal toxicity. These obstacles significantly limit the practical applications of IND and make that 10–20% of patients discontinue its use. Therefore, during the last three decades many attempts have been made to design novel formulations of IND aimed to increase its therapeutic benefits minimizing its adverse effects. In this review we summarize pharmacological information about IND and analyze its new lipid formulations and lipid bioconjugates as well as discuss their efficacy and potential application.https://www.mdpi.com/1420-3049/26/6/1576bioconjugatesindomethacinlipid-based formulationsprodrugsdrug-phospholipid conjugatesliposomes
spellingShingle Anna Gliszczyńska
Marta Nowaczyk
Lipid Formulations and Bioconjugation Strategies for Indomethacin Therapeutic Advances
Molecules
bioconjugates
indomethacin
lipid-based formulations
prodrugs
drug-phospholipid conjugates
liposomes
title Lipid Formulations and Bioconjugation Strategies for Indomethacin Therapeutic Advances
title_full Lipid Formulations and Bioconjugation Strategies for Indomethacin Therapeutic Advances
title_fullStr Lipid Formulations and Bioconjugation Strategies for Indomethacin Therapeutic Advances
title_full_unstemmed Lipid Formulations and Bioconjugation Strategies for Indomethacin Therapeutic Advances
title_short Lipid Formulations and Bioconjugation Strategies for Indomethacin Therapeutic Advances
title_sort lipid formulations and bioconjugation strategies for indomethacin therapeutic advances
topic bioconjugates
indomethacin
lipid-based formulations
prodrugs
drug-phospholipid conjugates
liposomes
url https://www.mdpi.com/1420-3049/26/6/1576
work_keys_str_mv AT annagliszczynska lipidformulationsandbioconjugationstrategiesforindomethacintherapeuticadvances
AT martanowaczyk lipidformulationsandbioconjugationstrategiesforindomethacintherapeuticadvances