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Design and Comparative Evaluation of Vancomycin HCl-Loaded Rosin-Based In Situ Forming Gel and Microparticles

Vancomycin hydrochloride (HCl) is a glycopeptide antibiotic used to treat serious or life-threatening infections, and it reduces plaque scores and gingivitis in periodontal patients. In this study, vancomycin HCl was incorporated into rosin in situ forming gel (ISG) and rosin in situ forming micropa...

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Autores principales: Chuenbarn, Tiraniti, Sirirak, Jitnapa, Tuntarawongsa, Sarun, Okonogi, Siriporn, Phaechamud, Thawatchai
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9031275/
https://www.ncbi.nlm.nih.gov/pubmed/35448132
http://dx.doi.org/10.3390/gels8040231
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author Chuenbarn, Tiraniti
Sirirak, Jitnapa
Tuntarawongsa, Sarun
Okonogi, Siriporn
Phaechamud, Thawatchai
author_facet Chuenbarn, Tiraniti
Sirirak, Jitnapa
Tuntarawongsa, Sarun
Okonogi, Siriporn
Phaechamud, Thawatchai
author_sort Chuenbarn, Tiraniti
collection PubMed
description Vancomycin hydrochloride (HCl) is a glycopeptide antibiotic used to treat serious or life-threatening infections, and it reduces plaque scores and gingivitis in periodontal patients. In this study, vancomycin HCl was incorporated into rosin in situ forming gel (ISG) and rosin in situ forming microparticles (ISM) to generate a local drug delivery system to treat periodontal disease. The physical properties of the ISG and ISM were measured, including pH, viscosity, injectability, adhesion properties, in-vitro transformation, and drug release. Moreover, the effectiveness of antimicrobial activity was tested using the agar-cup diffusion method against Staphylococcus aureus, Streptococcus mutans, Porphyromonas gingivalis, and Escherichia coli. Vancomycin HCl-loaded rosin-based ISG and ISM had a pH value in the range of 5.02–6.48 and exhibited the ease of injection with an injection force of less than 20 N. Additionally, the lubricity effect of the external oil phase of ISM promoted less work of injection than ISG and 40–60% rosin-based ISM showed good emulsion stability. The droplet size of emulsions containing 40%, 50%, and 60% rosin was 98.48 ± 16.11, 125.55 ± 4.75, and 137.80 ± 16.8 µm, respectively. Their obtained microparticles were significantly smaller in diameter, 78.63 ± 12.97, 93.81 ± 10.53, and 118.32 ± 15.61 µm, respectively, because the particles shrank due to the solvent loss from solvent exchange. Moreover, increasing the concentration of rosin increased the size of microparticles. After phase transformation, all formulations had better plasticity properties than elasticity; therefore, they could easily adapt to the specific shape of a patient’s gum cavity. Both developed ISG and ISM presented inhibition zones against S. mutans and P. gingivalis, with ISG presenting significantly more effectively against these two microbes (p < 0.05). The vancomycin HCl-loaded rosin ISG and ISM delayed drug release for 7 days with efficient antimicrobial activities; thus, they exhibit potential as the drug delivery systems for periodontitis treatment.
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spelling pubmed-90312752022-04-23 Design and Comparative Evaluation of Vancomycin HCl-Loaded Rosin-Based In Situ Forming Gel and Microparticles Chuenbarn, Tiraniti Sirirak, Jitnapa Tuntarawongsa, Sarun Okonogi, Siriporn Phaechamud, Thawatchai Gels Article Vancomycin hydrochloride (HCl) is a glycopeptide antibiotic used to treat serious or life-threatening infections, and it reduces plaque scores and gingivitis in periodontal patients. In this study, vancomycin HCl was incorporated into rosin in situ forming gel (ISG) and rosin in situ forming microparticles (ISM) to generate a local drug delivery system to treat periodontal disease. The physical properties of the ISG and ISM were measured, including pH, viscosity, injectability, adhesion properties, in-vitro transformation, and drug release. Moreover, the effectiveness of antimicrobial activity was tested using the agar-cup diffusion method against Staphylococcus aureus, Streptococcus mutans, Porphyromonas gingivalis, and Escherichia coli. Vancomycin HCl-loaded rosin-based ISG and ISM had a pH value in the range of 5.02–6.48 and exhibited the ease of injection with an injection force of less than 20 N. Additionally, the lubricity effect of the external oil phase of ISM promoted less work of injection than ISG and 40–60% rosin-based ISM showed good emulsion stability. The droplet size of emulsions containing 40%, 50%, and 60% rosin was 98.48 ± 16.11, 125.55 ± 4.75, and 137.80 ± 16.8 µm, respectively. Their obtained microparticles were significantly smaller in diameter, 78.63 ± 12.97, 93.81 ± 10.53, and 118.32 ± 15.61 µm, respectively, because the particles shrank due to the solvent loss from solvent exchange. Moreover, increasing the concentration of rosin increased the size of microparticles. After phase transformation, all formulations had better plasticity properties than elasticity; therefore, they could easily adapt to the specific shape of a patient’s gum cavity. Both developed ISG and ISM presented inhibition zones against S. mutans and P. gingivalis, with ISG presenting significantly more effectively against these two microbes (p < 0.05). The vancomycin HCl-loaded rosin ISG and ISM delayed drug release for 7 days with efficient antimicrobial activities; thus, they exhibit potential as the drug delivery systems for periodontitis treatment. MDPI 2022-04-08 /pmc/articles/PMC9031275/ /pubmed/35448132 http://dx.doi.org/10.3390/gels8040231 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Chuenbarn, Tiraniti
Sirirak, Jitnapa
Tuntarawongsa, Sarun
Okonogi, Siriporn
Phaechamud, Thawatchai
Design and Comparative Evaluation of Vancomycin HCl-Loaded Rosin-Based In Situ Forming Gel and Microparticles
title Design and Comparative Evaluation of Vancomycin HCl-Loaded Rosin-Based In Situ Forming Gel and Microparticles
title_full Design and Comparative Evaluation of Vancomycin HCl-Loaded Rosin-Based In Situ Forming Gel and Microparticles
title_fullStr Design and Comparative Evaluation of Vancomycin HCl-Loaded Rosin-Based In Situ Forming Gel and Microparticles
title_full_unstemmed Design and Comparative Evaluation of Vancomycin HCl-Loaded Rosin-Based In Situ Forming Gel and Microparticles
title_short Design and Comparative Evaluation of Vancomycin HCl-Loaded Rosin-Based In Situ Forming Gel and Microparticles
title_sort design and comparative evaluation of vancomycin hcl-loaded rosin-based in situ forming gel and microparticles
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9031275/
https://www.ncbi.nlm.nih.gov/pubmed/35448132
http://dx.doi.org/10.3390/gels8040231
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