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

Abstract

AimsThis research aimed to prepare and physically characterize methotrexate-encapsulated poly (n-methyl glycine) microspheres as a treatment option for rheumatoid arthritis. BackgroundRheumatoid 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. ObjectiveThe 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. MethodMethotrexate (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. ResultThe 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. ConclusionThe MTX-PSar Microsphere is a good option for treating RA despite the lack of in vivo action. OtherIt 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.