Rasagiline Mesylate

Varela A, et al. Archives of Cardiovascular Diseases Supplements, 2015, 7(1), 83-84.

Rasagiline Mesylate is primarily used for the treatment of neurodegenerative diseases like Parkinson's. However, its potential cardioprotective properties have garnered attention in recent studies. In this preclinical study, we investigated the effects of Rasagiline Mesylate in a rat model of myocardial infarction (MI).
The experimental design involved male Wistar rats (350-400g), where MI was induced via permanent ligation of the left anterior descending coronary artery. The rats were divided into three groups: Rasagiline-treated (R), control (C), and sham-operated (S). Rasagiline was administered intraperitoneally at 2 mg/kg daily for four weeks starting 24 hours post-MI induction. Cardiac function was monitored using echocardiography, while cardiac remodeling and cardiomyocyte damage were assessed through immunofluorescent microscopy.
Results showed that Rasagiline-treated rats exhibited significantly better systolic function, as indicated by fractional shortening (FS), compared to controls, at both 14 and 28 days post-MI. Notably, Rasagiline treatment also resulted in reduced collagen I deposition and less cardiomyocyte degeneration in the infarct border zone, suggesting a reduction in fibrosis and cellular damage. Additionally, apoptosis was markedly reduced in Rasagiline-treated animals, with a 65% decrease in the border zone and 58% reduction in the remote region.

Fernández M, et al. International Journal of Pharmaceutics, 2012, 438(1-2), 266-278.

Rasagiline mesylate (RM) was encapsulated into poly(lactic-co-glycolic acid) (PLGA) microspheres using two distinct formulation methods: oil-in-water (O/W) emulsion (Method A) and water-in-oil-in-water (W/O/W) double emulsion (Method B). The aim was to optimize drug loading, encapsulation efficiency, and release kinetics for controlled sustained drug delivery.
Method A (O/W Emulsion): In this approach, RM was dissolved in dichloromethane and emulsified into a PLGA solution using a vortex mixer and sonication. The O/W emulsion was subsequently emulsified in a PVA solution containing NaCl and stirred under controlled conditions to allow the organic solvent to evaporate. The resulting microspheres, after vacuum filtration and lyophilization, demonstrated a stable, two-week controlled release profile. The method was efficient in achieving high encapsulation rates and consistent drug release.
Method B (W/O/W Double Emulsion): In the W/O/W double emulsion method, RM was initially dissolved in PBS and emulsified into dichloromethane containing PLGA. This primary W/O emulsion was then further emulsified into an external PVA solution under high-shear conditions. The microspheres were recovered and freeze-dried, yielding a controlled drug release, though with slightly lower efficiency than Method A.
Both techniques produced viable RM-loaded PLGA microspheres, with Method A offering superior process yield and consistent drug release, making it the preferable method for the sustained delivery of Rasagiline Mesylate in therapeutic applications.

Mahajan S, et al. Journal of Drug Delivery Science and Technology, 2024, 95, 105549.

The RM@CS/B-GP-GO hydrogel was designed to provide a new approach for delivering Rasagiline Mesylate (RM) via the nasal route. Below are the steps for preparing a 10 mL hydrogel formulation of RM@CS/B-GP-GO:
Preparation of RM Solution: Ten milligrams of RM were dissolved in 4 mL of 0.1 M acetic acid. The solution was stirred on a magnetic stirrer until a clear solution was obtained.
Preparation of GO Dispersion: Various concentrations of graphene oxide (GO) (0.5 mg/mL, 1 mg/mL, 1.5 mg/mL, and 2 mg/mL) were dissolved in 4 mL of 0.1 M acetic acid. A probe sonicator (PCI Analytics, Mumbai, India) was used for 10 cycles to achieve a well-dispersed GO solution.
Preparation of B-GP Solution: Four hundred sixty milligrams of B-GP were dissolved in 2 mL of distilled water to form a B-GP solution.
Hydrogel Formation: The RM solution was gradually added to the GO dispersions (0.5 mg/mL and 1 mg/mL) while stirring at 200 RPM for 5 minutes. Next, 125 mg of chitosan (CS) was added to the mixture, and stirring was continued for 12 hours at room temperature until a homogeneous solution was obtained.
Final Hydrogel Formation: The B-GP solution was then added dropwise into the RM@CS-GO mixture while stirring at 300 RPM in an ice bath for 20 minutes.

ElShagea HN, et al. Journal of Drug Delivery Science and Technology, 2024, 92, 105369.

This study focuses on the preparation of novasomal formulations loaded with Rasagiline mesylate (RSM), with significant improvements made by incorporating terpenes during the manufacturing process. The aim is to enhance transdermal permeation, allowing the active ingredient to penetrate the skin and enter systemic circulation.
RSM, cholesterol, surfactant (Span 80), and free fatty acid (stearic acid), with or without terpenes, were dissolved in 2 mL of ethanol. The solution was subjected to sonication at 60°C using a water bath ultrasonic generator. The resulting ethanol solution was then slowly added dropwise into phosphate-buffered saline (PBS, pH 7.4) under stirring (500 rpm) on a magnetic stirrer for 30 minutes, ensuring complete evaporation of the ethanol and formation of the novasomes. The novasomal dispersion was further sonicated for 10 minutes at 25°C using the ultrasonic generator to reduce particle size. The prepared formulation was stored at 4°C for further studies.