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Clarithromycin-Loaded Submicron-Sized Carriers: Pharmacokinetics and Pharmacodynamic Evaluation
The current study aims to improve clarithromycin bioavailability and effectiveness in complicated intra-abdominal infection management. Therefore, clarithromycin-loaded submicron dual lipid carriers (CLA-DLCs) were developed via hot high shear homogenization technique and evaluated for colloidal par...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10179782/ https://www.ncbi.nlm.nih.gov/pubmed/37176475 http://dx.doi.org/10.3390/ma16093593 |
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author | Rawat, Reetika Chouhan, Raghuraj Singh Sadhu, Veera Sharma, Manu |
author_facet | Rawat, Reetika Chouhan, Raghuraj Singh Sadhu, Veera Sharma, Manu |
author_sort | Rawat, Reetika |
collection | PubMed |
description | The current study aims to improve clarithromycin bioavailability and effectiveness in complicated intra-abdominal infection management. Therefore, clarithromycin-loaded submicron dual lipid carriers (CLA-DLCs) were developed via hot high shear homogenization technique and evaluated for colloidal parameters, release behavior, stability study, and in-vitro antibiofilm activity. Bioavailability and therapeutic efficacy of optimized formulation on hampering cytokines storm induction was determined in E. coli-induced peritonitis. The developed CLA-DLCs (particle size 326.19 ± 24.14 nm, zeta potential −31.34 ± 2.81 mV, and entrapment efficiency 85.78 ± 4.01%) exhibited smooth spherical shapes and sustained in vitro release profiles. Long-term stability study of optimized CLA-DLCs ensured maintenance of colloidal parameters for 1 year at room temperature. In vitro antimicrobial studies revealed 3.43-fold higher anti-biofilm activity of CLA-DLCs compared with clarithromycin. In addition, the relative bioavailability of CLA-DLCs was enhanced 5.89-fold compared to pure drug in rats. The remarkable decrease in microbial burden in blood as well as tissues, along with oxidative stress markers (lipid peroxidation, myeloperoxidase activity, and carbonylated protein level) and immunological markers (total leukocyte count, neutrophil migration, NO, TNF-, and IL-6) on treatment with CLA-DLCs enhanced the survival in a rat model of peritonitis compared with the pure drug and untreated groups. In conclusion, CLA-DLCs hold promising potential in management of intra-abdominal infections and prevention of associated complications. |
format | Online Article Text |
id | pubmed-10179782 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-101797822023-05-13 Clarithromycin-Loaded Submicron-Sized Carriers: Pharmacokinetics and Pharmacodynamic Evaluation Rawat, Reetika Chouhan, Raghuraj Singh Sadhu, Veera Sharma, Manu Materials (Basel) Article The current study aims to improve clarithromycin bioavailability and effectiveness in complicated intra-abdominal infection management. Therefore, clarithromycin-loaded submicron dual lipid carriers (CLA-DLCs) were developed via hot high shear homogenization technique and evaluated for colloidal parameters, release behavior, stability study, and in-vitro antibiofilm activity. Bioavailability and therapeutic efficacy of optimized formulation on hampering cytokines storm induction was determined in E. coli-induced peritonitis. The developed CLA-DLCs (particle size 326.19 ± 24.14 nm, zeta potential −31.34 ± 2.81 mV, and entrapment efficiency 85.78 ± 4.01%) exhibited smooth spherical shapes and sustained in vitro release profiles. Long-term stability study of optimized CLA-DLCs ensured maintenance of colloidal parameters for 1 year at room temperature. In vitro antimicrobial studies revealed 3.43-fold higher anti-biofilm activity of CLA-DLCs compared with clarithromycin. In addition, the relative bioavailability of CLA-DLCs was enhanced 5.89-fold compared to pure drug in rats. The remarkable decrease in microbial burden in blood as well as tissues, along with oxidative stress markers (lipid peroxidation, myeloperoxidase activity, and carbonylated protein level) and immunological markers (total leukocyte count, neutrophil migration, NO, TNF-, and IL-6) on treatment with CLA-DLCs enhanced the survival in a rat model of peritonitis compared with the pure drug and untreated groups. In conclusion, CLA-DLCs hold promising potential in management of intra-abdominal infections and prevention of associated complications. MDPI 2023-05-08 /pmc/articles/PMC10179782/ /pubmed/37176475 http://dx.doi.org/10.3390/ma16093593 Text en © 2023 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 Rawat, Reetika Chouhan, Raghuraj Singh Sadhu, Veera Sharma, Manu Clarithromycin-Loaded Submicron-Sized Carriers: Pharmacokinetics and Pharmacodynamic Evaluation |
title | Clarithromycin-Loaded Submicron-Sized Carriers: Pharmacokinetics and Pharmacodynamic Evaluation |
title_full | Clarithromycin-Loaded Submicron-Sized Carriers: Pharmacokinetics and Pharmacodynamic Evaluation |
title_fullStr | Clarithromycin-Loaded Submicron-Sized Carriers: Pharmacokinetics and Pharmacodynamic Evaluation |
title_full_unstemmed | Clarithromycin-Loaded Submicron-Sized Carriers: Pharmacokinetics and Pharmacodynamic Evaluation |
title_short | Clarithromycin-Loaded Submicron-Sized Carriers: Pharmacokinetics and Pharmacodynamic Evaluation |
title_sort | clarithromycin-loaded submicron-sized carriers: pharmacokinetics and pharmacodynamic evaluation |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10179782/ https://www.ncbi.nlm.nih.gov/pubmed/37176475 http://dx.doi.org/10.3390/ma16093593 |
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