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Chitosan Encapsulated Meloxicam Nanoparticles for Sustained Drug Delivery Applications: Preparation, Characterization, and Pharmacokinetics in Wistar Rats

Meloxicam (MLX) is currently used in the therapeutic management of both acute and chronic inflammatory disorders such as pain, injuries, osteoarthritis, and rheumatoid arthritis in both humans and animals. Gastrointestinal toxicity and occasional renal toxicity were observed in patients taking it fo...

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Autores principales: Yegireddy, Muralidhar, Nadoor, Prakash, Rao, Suguna, Hanumanthu, Pavithra Balekatte, Rajashekaraiah, Rashmi, Ramachandrappa, Santhosh Chickankandahalli, Halemani, Girish Mallikarjun, Mannem, Sravanthi, Prasad, Tollamadugu Naga Venkata Krishna Vara, Ubaradka, Sunilchandra
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9658985/
https://www.ncbi.nlm.nih.gov/pubmed/36364138
http://dx.doi.org/10.3390/molecules27217312
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author Yegireddy, Muralidhar
Nadoor, Prakash
Rao, Suguna
Hanumanthu, Pavithra Balekatte
Rajashekaraiah, Rashmi
Ramachandrappa, Santhosh Chickankandahalli
Halemani, Girish Mallikarjun
Mannem, Sravanthi
Prasad, Tollamadugu Naga Venkata Krishna Vara
Ubaradka, Sunilchandra
author_facet Yegireddy, Muralidhar
Nadoor, Prakash
Rao, Suguna
Hanumanthu, Pavithra Balekatte
Rajashekaraiah, Rashmi
Ramachandrappa, Santhosh Chickankandahalli
Halemani, Girish Mallikarjun
Mannem, Sravanthi
Prasad, Tollamadugu Naga Venkata Krishna Vara
Ubaradka, Sunilchandra
author_sort Yegireddy, Muralidhar
collection PubMed
description Meloxicam (MLX) is currently used in the therapeutic management of both acute and chronic inflammatory disorders such as pain, injuries, osteoarthritis, and rheumatoid arthritis in both humans and animals. Gastrointestinal toxicity and occasional renal toxicity were observed in patients taking it for a long-term period. Meloxicam’s late attainment of peak plasma concentration results in a slow onset of action. The goal of the current study was to prepare and characterize chitosan encapsulated meloxicam nanoparticles (CEMNPs) with high bioavailability and less gastro intestinal toxicity in order to prevent such issues. The size of the prepared CEMNPs was approximately 110–220 nm with a zetapotential of +39.9 mV and polydispersity index of 0.268, suggesting that they were uniformly dispersed nanoparticles. The FTIR and UV-Vis spectroscopy have confirmed the presence of MLX in the prepared CEMNPs. The pharmacokinetics have been studied with three groups of male Wistar rats receiving either of the treatments, viz., 4 mg·kg(−1) of MLX and 1 or 4 mg·kg(−1) of CEMNPs. Plasma samples were collected until 48 h post administration, and concentrations of MLX were quantified by using reverse (C(18)) phase HPLC. Non-compartmental analysis was applied to determine pharmacokinetic variables. Upon oral administration, the maximum concentration (C(max)) was reached in 4 h for CEMNPs and 6 h for MLX. The mean area under the plasma MLX concentration-time curve from ‘zero’ to infinity (AUC(0–∞)), half-life (t(1/2β)), and mean resident time (MRT) of 1 mg·kg(−1) of CEMNPs was 1.4-, 2-, and 1.8-fold greater than 4 mg·kg(−1) of MLX. The prepared CEMNPs demonstrated quicker absorption and prolonged release along with a significant improvement in the bioavailability of MLX, paving a prospective path for the development of drugs with enhanced bioavailability with less side effects.
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spelling pubmed-96589852022-11-15 Chitosan Encapsulated Meloxicam Nanoparticles for Sustained Drug Delivery Applications: Preparation, Characterization, and Pharmacokinetics in Wistar Rats Yegireddy, Muralidhar Nadoor, Prakash Rao, Suguna Hanumanthu, Pavithra Balekatte Rajashekaraiah, Rashmi Ramachandrappa, Santhosh Chickankandahalli Halemani, Girish Mallikarjun Mannem, Sravanthi Prasad, Tollamadugu Naga Venkata Krishna Vara Ubaradka, Sunilchandra Molecules Article Meloxicam (MLX) is currently used in the therapeutic management of both acute and chronic inflammatory disorders such as pain, injuries, osteoarthritis, and rheumatoid arthritis in both humans and animals. Gastrointestinal toxicity and occasional renal toxicity were observed in patients taking it for a long-term period. Meloxicam’s late attainment of peak plasma concentration results in a slow onset of action. The goal of the current study was to prepare and characterize chitosan encapsulated meloxicam nanoparticles (CEMNPs) with high bioavailability and less gastro intestinal toxicity in order to prevent such issues. The size of the prepared CEMNPs was approximately 110–220 nm with a zetapotential of +39.9 mV and polydispersity index of 0.268, suggesting that they were uniformly dispersed nanoparticles. The FTIR and UV-Vis spectroscopy have confirmed the presence of MLX in the prepared CEMNPs. The pharmacokinetics have been studied with three groups of male Wistar rats receiving either of the treatments, viz., 4 mg·kg(−1) of MLX and 1 or 4 mg·kg(−1) of CEMNPs. Plasma samples were collected until 48 h post administration, and concentrations of MLX were quantified by using reverse (C(18)) phase HPLC. Non-compartmental analysis was applied to determine pharmacokinetic variables. Upon oral administration, the maximum concentration (C(max)) was reached in 4 h for CEMNPs and 6 h for MLX. The mean area under the plasma MLX concentration-time curve from ‘zero’ to infinity (AUC(0–∞)), half-life (t(1/2β)), and mean resident time (MRT) of 1 mg·kg(−1) of CEMNPs was 1.4-, 2-, and 1.8-fold greater than 4 mg·kg(−1) of MLX. The prepared CEMNPs demonstrated quicker absorption and prolonged release along with a significant improvement in the bioavailability of MLX, paving a prospective path for the development of drugs with enhanced bioavailability with less side effects. MDPI 2022-10-27 /pmc/articles/PMC9658985/ /pubmed/36364138 http://dx.doi.org/10.3390/molecules27217312 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
Yegireddy, Muralidhar
Nadoor, Prakash
Rao, Suguna
Hanumanthu, Pavithra Balekatte
Rajashekaraiah, Rashmi
Ramachandrappa, Santhosh Chickankandahalli
Halemani, Girish Mallikarjun
Mannem, Sravanthi
Prasad, Tollamadugu Naga Venkata Krishna Vara
Ubaradka, Sunilchandra
Chitosan Encapsulated Meloxicam Nanoparticles for Sustained Drug Delivery Applications: Preparation, Characterization, and Pharmacokinetics in Wistar Rats
title Chitosan Encapsulated Meloxicam Nanoparticles for Sustained Drug Delivery Applications: Preparation, Characterization, and Pharmacokinetics in Wistar Rats
title_full Chitosan Encapsulated Meloxicam Nanoparticles for Sustained Drug Delivery Applications: Preparation, Characterization, and Pharmacokinetics in Wistar Rats
title_fullStr Chitosan Encapsulated Meloxicam Nanoparticles for Sustained Drug Delivery Applications: Preparation, Characterization, and Pharmacokinetics in Wistar Rats
title_full_unstemmed Chitosan Encapsulated Meloxicam Nanoparticles for Sustained Drug Delivery Applications: Preparation, Characterization, and Pharmacokinetics in Wistar Rats
title_short Chitosan Encapsulated Meloxicam Nanoparticles for Sustained Drug Delivery Applications: Preparation, Characterization, and Pharmacokinetics in Wistar Rats
title_sort chitosan encapsulated meloxicam nanoparticles for sustained drug delivery applications: preparation, characterization, and pharmacokinetics in wistar rats
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9658985/
https://www.ncbi.nlm.nih.gov/pubmed/36364138
http://dx.doi.org/10.3390/molecules27217312
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