Antimicrobial Preservatives in Cyclodextrin-Containing Drug Formulations

In general, antimicrobial preservatives are essential components of multidose pharmaceutical formulations to prevent microbial growth and contamination, many of which contain lipophilic and poorly water-soluble drugs in need of solubilizing excipients, such as cyclodextrins (CDs). However, CDs frequ...

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Main Authors: Phatsawee Jansook, Hákon Hrafn Sigurdsson, Frédéric Pilotaz, Thorsteinn Loftsson
Format: Article
Language:English
Published: MDPI AG 2024-12-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/16/12/1601
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author Phatsawee Jansook
Hákon Hrafn Sigurdsson
Frédéric Pilotaz
Thorsteinn Loftsson
author_facet Phatsawee Jansook
Hákon Hrafn Sigurdsson
Frédéric Pilotaz
Thorsteinn Loftsson
author_sort Phatsawee Jansook
collection DOAJ
description In general, antimicrobial preservatives are essential components of multidose pharmaceutical formulations to prevent microbial growth and contamination, many of which contain lipophilic and poorly water-soluble drugs in need of solubilizing excipients, such as cyclodextrins (CDs). However, CDs frequently reduce or even abolish the antimicrobial activities of commonly used pharmaceutical preservatives. The degree of inactivation depends on the CD complexation of the preservatives, which in turn depends on their chemical structure and physiochemical properties. In general, lipophilic preservatives are more likely to be inactivated; however, CDs are also known to inactivate highly water-soluble preservatives. In some drug formulations, preservative inactivation has been offset by including excipients that possess some antimicrobial activity on their own. In this review, we explain how CDs interact with some commonly used pharmaceutical preservatives and why some preservatives are more susceptible to CD inactivation than others are.
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id doaj-art-148e49e48bb3496e8ffe6a7de48e9c23
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language English
publishDate 2024-12-01
publisher MDPI AG
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series Pharmaceutics
spelling doaj-art-148e49e48bb3496e8ffe6a7de48e9c232025-08-20T02:43:42ZengMDPI AGPharmaceutics1999-49232024-12-011612160110.3390/pharmaceutics16121601Antimicrobial Preservatives in Cyclodextrin-Containing Drug FormulationsPhatsawee Jansook0Hákon Hrafn Sigurdsson1Frédéric Pilotaz2Thorsteinn Loftsson3Faculty of Pharmaceutical Sciences, Chulalongkorn University, 254 Payathai Road, Pathumwan, Bangkok 10330, ThailandFaculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, IcelandHorus-Pharma, Département des Opérations Industrielles, 22, allée Camille-Muffat, bât. Inedi 5, 06200 Nice, FranceFaculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, IcelandIn general, antimicrobial preservatives are essential components of multidose pharmaceutical formulations to prevent microbial growth and contamination, many of which contain lipophilic and poorly water-soluble drugs in need of solubilizing excipients, such as cyclodextrins (CDs). However, CDs frequently reduce or even abolish the antimicrobial activities of commonly used pharmaceutical preservatives. The degree of inactivation depends on the CD complexation of the preservatives, which in turn depends on their chemical structure and physiochemical properties. In general, lipophilic preservatives are more likely to be inactivated; however, CDs are also known to inactivate highly water-soluble preservatives. In some drug formulations, preservative inactivation has been offset by including excipients that possess some antimicrobial activity on their own. In this review, we explain how CDs interact with some commonly used pharmaceutical preservatives and why some preservatives are more susceptible to CD inactivation than others are.https://www.mdpi.com/1999-4923/16/12/1601antimicrobial preservativecyclodextrininactivationantimicrobial efficacy enhancer
spellingShingle Phatsawee Jansook
Hákon Hrafn Sigurdsson
Frédéric Pilotaz
Thorsteinn Loftsson
Antimicrobial Preservatives in Cyclodextrin-Containing Drug Formulations
Pharmaceutics
antimicrobial preservative
cyclodextrin
inactivation
antimicrobial efficacy enhancer
title Antimicrobial Preservatives in Cyclodextrin-Containing Drug Formulations
title_full Antimicrobial Preservatives in Cyclodextrin-Containing Drug Formulations
title_fullStr Antimicrobial Preservatives in Cyclodextrin-Containing Drug Formulations
title_full_unstemmed Antimicrobial Preservatives in Cyclodextrin-Containing Drug Formulations
title_short Antimicrobial Preservatives in Cyclodextrin-Containing Drug Formulations
title_sort antimicrobial preservatives in cyclodextrin containing drug formulations
topic antimicrobial preservative
cyclodextrin
inactivation
antimicrobial efficacy enhancer
url https://www.mdpi.com/1999-4923/16/12/1601
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AT hakonhrafnsigurdsson antimicrobialpreservativesincyclodextrincontainingdrugformulations
AT fredericpilotaz antimicrobialpreservativesincyclodextrincontainingdrugformulations
AT thorsteinnloftsson antimicrobialpreservativesincyclodextrincontainingdrugformulations