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

Authors :
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
Source :
Molecules; Nov2022, Vol. 27 Issue 21, p7312, 17p
Publication Year :
2022

Abstract

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<superscript>−1</superscript> of MLX and 1 or 4 mg·kg<superscript>−1</superscript> of CEMNPs. Plasma samples were collected until 48 h post administration, and concentrations of MLX were quantified by using reverse (C<subscript>18</subscript>) phase HPLC. Non-compartmental analysis was applied to determine pharmacokinetic variables. Upon oral administration, the maximum concentration (C<subscript>max</subscript>) 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<subscript>0–∞</subscript>), half-life (t<subscript>1/2β</subscript>), and mean resident time (MRT) of 1 mg·kg<superscript>−1</superscript> of CEMNPs was 1.4-, 2-, and 1.8-fold greater than 4 mg·kg<superscript>−1</superscript> 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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
14203049
Volume :
27
Issue :
21
Database :
Complementary Index
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
160217751
Full Text :
https://doi.org/10.3390/molecules27217312