Insight in Superiority of the Hydrophobized Gentamycin in Terms of Antibiotics Delivery to Bone Tissue

Bone infections are a serious problem to cure, as systemic administration of antibiotics is not very effective due to poor bone vascularization. Therefore, many drug delivery systems are investigated to solve this problem. One of the potential solutions is the delivery of antibiotics from poly(L-act...

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Main Authors: Konrad Kwiecień, Iwona Pudełko, Karolina Knap, Katarzyna Reczyńska-Kolman, Małgorzata Krok-Borkowicz, Dorota Ochońska, Monika Brzychczy-Włoch, Elżbieta Pamuła
Format: Article
Language:English
Published: MDPI AG 2022-10-01
Series:International Journal of Molecular Sciences
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Online Access:https://www.mdpi.com/1422-0067/23/20/12077
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author Konrad Kwiecień
Iwona Pudełko
Karolina Knap
Katarzyna Reczyńska-Kolman
Małgorzata Krok-Borkowicz
Dorota Ochońska
Monika Brzychczy-Włoch
Elżbieta Pamuła
author_facet Konrad Kwiecień
Iwona Pudełko
Karolina Knap
Katarzyna Reczyńska-Kolman
Małgorzata Krok-Borkowicz
Dorota Ochońska
Monika Brzychczy-Włoch
Elżbieta Pamuła
author_sort Konrad Kwiecień
collection DOAJ
description Bone infections are a serious problem to cure, as systemic administration of antibiotics is not very effective due to poor bone vascularization. Therefore, many drug delivery systems are investigated to solve this problem. One of the potential solutions is the delivery of antibiotics from poly(L-actide-co-glycolide) (PLGA) nanoparticles suspended in the gellan gum injectable hydrogel. However, the loading capacity and release kinetics of the system based on hydrophilic drugs (e.g., gentamycin) and hydrophobic polymers (e.g., PLGA) may not always be satisfying. To solve this problem, we decided to use hydrophobized gentamycin obtained by ion-pairing with dioctyl sulfosuccinate sodium salt (AOT). Herein, we present a comparison of the PLGA nanoparticles loaded with hydrophobic or hydrophilic gentamycin and suspended in the hydrogel in terms of physicochemical properties, drug loading capacity, release profiles, cytocompatibility, and antibacterial properties. The results showed that hydrophobic gentamycin may be combined in different formulations with the hydrophilic one and is superior in terms of encapsulation efficiency, drug loading, release, and antibacterial efficacy with no negative effect on the NPs morphology or hydrogel features. However, the cytocompatibility of hydrophobic gentamycin might be lower, consequently more extensive study on its biological properties should be provided to evaluate a safe dose.
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spelling doaj.art-0a8d599592824a06b89319b56ea421e62023-11-24T00:28:22ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672022-10-0123201207710.3390/ijms232012077Insight in Superiority of the Hydrophobized Gentamycin in Terms of Antibiotics Delivery to Bone TissueKonrad Kwiecień0Iwona Pudełko1Karolina Knap2Katarzyna Reczyńska-Kolman3Małgorzata Krok-Borkowicz4Dorota Ochońska5Monika Brzychczy-Włoch6Elżbieta Pamuła7Department of Biomaterials and Composites, Faculty of Materials Science and Ceramics, AGH University of Science and Technology, Al. Mickiewicza 30, 30-059 Kraków, PolandDepartment of Biomaterials and Composites, Faculty of Materials Science and Ceramics, AGH University of Science and Technology, Al. Mickiewicza 30, 30-059 Kraków, PolandDepartment of Biomaterials and Composites, Faculty of Materials Science and Ceramics, AGH University of Science and Technology, Al. Mickiewicza 30, 30-059 Kraków, PolandDepartment of Biomaterials and Composites, Faculty of Materials Science and Ceramics, AGH University of Science and Technology, Al. Mickiewicza 30, 30-059 Kraków, PolandDepartment of Biomaterials and Composites, Faculty of Materials Science and Ceramics, AGH University of Science and Technology, Al. Mickiewicza 30, 30-059 Kraków, PolandDepartment of Molecular Medical Microbiology, Chair of Microbiology, Faculty of Medicine, Jagiellonian University Medical College, 18 Czysta Street, 31-121 Kraków, PolandDepartment of Molecular Medical Microbiology, Chair of Microbiology, Faculty of Medicine, Jagiellonian University Medical College, 18 Czysta Street, 31-121 Kraków, PolandDepartment of Biomaterials and Composites, Faculty of Materials Science and Ceramics, AGH University of Science and Technology, Al. Mickiewicza 30, 30-059 Kraków, PolandBone infections are a serious problem to cure, as systemic administration of antibiotics is not very effective due to poor bone vascularization. Therefore, many drug delivery systems are investigated to solve this problem. One of the potential solutions is the delivery of antibiotics from poly(L-actide-co-glycolide) (PLGA) nanoparticles suspended in the gellan gum injectable hydrogel. However, the loading capacity and release kinetics of the system based on hydrophilic drugs (e.g., gentamycin) and hydrophobic polymers (e.g., PLGA) may not always be satisfying. To solve this problem, we decided to use hydrophobized gentamycin obtained by ion-pairing with dioctyl sulfosuccinate sodium salt (AOT). Herein, we present a comparison of the PLGA nanoparticles loaded with hydrophobic or hydrophilic gentamycin and suspended in the hydrogel in terms of physicochemical properties, drug loading capacity, release profiles, cytocompatibility, and antibacterial properties. The results showed that hydrophobic gentamycin may be combined in different formulations with the hydrophilic one and is superior in terms of encapsulation efficiency, drug loading, release, and antibacterial efficacy with no negative effect on the NPs morphology or hydrogel features. However, the cytocompatibility of hydrophobic gentamycin might be lower, consequently more extensive study on its biological properties should be provided to evaluate a safe dose.https://www.mdpi.com/1422-0067/23/20/12077hydrogelsbone tissuenanoparticlesPLGAgentamycinAOT
spellingShingle Konrad Kwiecień
Iwona Pudełko
Karolina Knap
Katarzyna Reczyńska-Kolman
Małgorzata Krok-Borkowicz
Dorota Ochońska
Monika Brzychczy-Włoch
Elżbieta Pamuła
Insight in Superiority of the Hydrophobized Gentamycin in Terms of Antibiotics Delivery to Bone Tissue
International Journal of Molecular Sciences
hydrogels
bone tissue
nanoparticles
PLGA
gentamycin
AOT
title Insight in Superiority of the Hydrophobized Gentamycin in Terms of Antibiotics Delivery to Bone Tissue
title_full Insight in Superiority of the Hydrophobized Gentamycin in Terms of Antibiotics Delivery to Bone Tissue
title_fullStr Insight in Superiority of the Hydrophobized Gentamycin in Terms of Antibiotics Delivery to Bone Tissue
title_full_unstemmed Insight in Superiority of the Hydrophobized Gentamycin in Terms of Antibiotics Delivery to Bone Tissue
title_short Insight in Superiority of the Hydrophobized Gentamycin in Terms of Antibiotics Delivery to Bone Tissue
title_sort insight in superiority of the hydrophobized gentamycin in terms of antibiotics delivery to bone tissue
topic hydrogels
bone tissue
nanoparticles
PLGA
gentamycin
AOT
url https://www.mdpi.com/1422-0067/23/20/12077
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