Preparation and physical characterization of Methotrexate encapsulated poly (n-methyl glycine) microspheres for the Rheumatoid arthritis treatment option

Aims: This research aimed to prepare and physically characterize methotrexate-encapsulated poly (n-methyl glycine) microspheres as a treatment option for rheumatoid arthritis. Background: Rheumatoid arthritis is an autoimmune disease that leads to cartilage destruction, synovial joint inflammation,...

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Main Authors: Rahul Shah, Sankha Bhattacharya
Format: Article
Language:English
Published: Elsevier 2023-01-01
Series:Results in Chemistry
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S2211715623001145
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author Rahul Shah
Sankha Bhattacharya
author_facet Rahul Shah
Sankha Bhattacharya
author_sort Rahul Shah
collection DOAJ
description Aims: This research aimed to prepare and physically characterize methotrexate-encapsulated poly (n-methyl glycine) microspheres as a treatment option for rheumatoid arthritis. Background: Rheumatoid arthritis is an autoimmune disease that leads to cartilage destruction, synovial joint inflammation, and bacterial joint/bone infections. Methotrexate (MTX), commonly used in rheumatoid arthritis (RA), has severe adverse effects. Therefore, a reliable drug delivery system is required to control the release of Methotrexate during the treatment of Rheumatoid arthritis. Objective: The primary goal of this study was to develop and characterise methotrexate-loaded polysarcosine microspheres (MTX-PSar Microspheres), as well as to examine their physical characteristics, pharmacodynamics, and anti-rheumatic study effects. Method: Methotrexate (MTX) loaded Polysarcosine (PSar) Microsphere was developed using Mannitol, Magnesium hydroxide, Dichloromethane, Aqueous polyvinyl alcohol and Chitosan hydrochloride. The MTX-PSar Microsphere was developed by w/o/w multiple emulsions method in the current study to reduce inflammation and disease progression/joint stiffness caused by Rheumatoid Arthritis. FTIR, HPLC, XRD, DSC, and SEM were used to evaluate the physical properties of MTX-PSar Microspheres. Result: The physicochemical characterizations of microparticles by Fourier Transform Infrared Spectroscopy and X-Ray Diffraction have shown that drug encapsulated in the microparticles and lost its crystalline nature. The particle size, entrapment efficacy, reported in the range of 10–20 µm, 86.37 ± 0.65 %. Even after one month, the microsphere’s particle size maintained its spherical shape In-vitro drug release, pharmacodynamics study shows good anti-rheumatic study effects. Conclusion: The MTX-PSar Microsphere is a good option for treating RA despite the lack of in vivo action. Other: It is hoped that in future studies, Methotrexate-loaded polysarcosine microspheres (MTX-PSar Microsphere) will be used to conjugate ligands, and hence active targeting in rheumatoid arthritis would be possible.
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spelling doaj.art-184c77aa55834340a23a3a672b5c99382023-06-21T06:52:22ZengElsevierResults in Chemistry2211-71562023-01-015100875Preparation and physical characterization of Methotrexate encapsulated poly (n-methyl glycine) microspheres for the Rheumatoid arthritis treatment optionRahul Shah0Sankha Bhattacharya1Department of Pharmaceutics, School of Pharmacy & Technology Management, SVKM’s NMIMS Deemed-to-be University, Shirpur, Maharashtra 425405, IndiaCorresponding author.; Department of Pharmaceutics, School of Pharmacy & Technology Management, SVKM’s NMIMS Deemed-to-be University, Shirpur, Maharashtra 425405, IndiaAims: This research aimed to prepare and physically characterize methotrexate-encapsulated poly (n-methyl glycine) microspheres as a treatment option for rheumatoid arthritis. Background: Rheumatoid arthritis is an autoimmune disease that leads to cartilage destruction, synovial joint inflammation, and bacterial joint/bone infections. Methotrexate (MTX), commonly used in rheumatoid arthritis (RA), has severe adverse effects. Therefore, a reliable drug delivery system is required to control the release of Methotrexate during the treatment of Rheumatoid arthritis. Objective: The primary goal of this study was to develop and characterise methotrexate-loaded polysarcosine microspheres (MTX-PSar Microspheres), as well as to examine their physical characteristics, pharmacodynamics, and anti-rheumatic study effects. Method: Methotrexate (MTX) loaded Polysarcosine (PSar) Microsphere was developed using Mannitol, Magnesium hydroxide, Dichloromethane, Aqueous polyvinyl alcohol and Chitosan hydrochloride. The MTX-PSar Microsphere was developed by w/o/w multiple emulsions method in the current study to reduce inflammation and disease progression/joint stiffness caused by Rheumatoid Arthritis. FTIR, HPLC, XRD, DSC, and SEM were used to evaluate the physical properties of MTX-PSar Microspheres. Result: The physicochemical characterizations of microparticles by Fourier Transform Infrared Spectroscopy and X-Ray Diffraction have shown that drug encapsulated in the microparticles and lost its crystalline nature. The particle size, entrapment efficacy, reported in the range of 10–20 µm, 86.37 ± 0.65 %. Even after one month, the microsphere’s particle size maintained its spherical shape In-vitro drug release, pharmacodynamics study shows good anti-rheumatic study effects. Conclusion: The MTX-PSar Microsphere is a good option for treating RA despite the lack of in vivo action. Other: It is hoped that in future studies, Methotrexate-loaded polysarcosine microspheres (MTX-PSar Microsphere) will be used to conjugate ligands, and hence active targeting in rheumatoid arthritis would be possible.http://www.sciencedirect.com/science/article/pii/S2211715623001145Rheumatoid ArthritisMethotrexatePolysarcosineMicrospheresPharmacodynamics studyCarrageenan-induced rat paw oedema
spellingShingle Rahul Shah
Sankha Bhattacharya
Preparation and physical characterization of Methotrexate encapsulated poly (n-methyl glycine) microspheres for the Rheumatoid arthritis treatment option
Results in Chemistry
Rheumatoid Arthritis
Methotrexate
Polysarcosine
Microspheres
Pharmacodynamics study
Carrageenan-induced rat paw oedema
title Preparation and physical characterization of Methotrexate encapsulated poly (n-methyl glycine) microspheres for the Rheumatoid arthritis treatment option
title_full Preparation and physical characterization of Methotrexate encapsulated poly (n-methyl glycine) microspheres for the Rheumatoid arthritis treatment option
title_fullStr Preparation and physical characterization of Methotrexate encapsulated poly (n-methyl glycine) microspheres for the Rheumatoid arthritis treatment option
title_full_unstemmed Preparation and physical characterization of Methotrexate encapsulated poly (n-methyl glycine) microspheres for the Rheumatoid arthritis treatment option
title_short Preparation and physical characterization of Methotrexate encapsulated poly (n-methyl glycine) microspheres for the Rheumatoid arthritis treatment option
title_sort preparation and physical characterization of methotrexate encapsulated poly n methyl glycine microspheres for the rheumatoid arthritis treatment option
topic Rheumatoid Arthritis
Methotrexate
Polysarcosine
Microspheres
Pharmacodynamics study
Carrageenan-induced rat paw oedema
url http://www.sciencedirect.com/science/article/pii/S2211715623001145
work_keys_str_mv AT rahulshah preparationandphysicalcharacterizationofmethotrexateencapsulatedpolynmethylglycinemicrospheresfortherheumatoidarthritistreatmentoption
AT sankhabhattacharya preparationandphysicalcharacterizationofmethotrexateencapsulatedpolynmethylglycinemicrospheresfortherheumatoidarthritistreatmentoption