Enhanced transdermal permeation of rasagiline mesylate nanoparticles: design, optimization, and effect of binary combinations of solvent systems across biological membrane

Abstract

Rasagiline mesylate (RM) used as first-line agent for Parkinsonism exhibit low oral-bioavailability and extensive hepatic first-pass metabolism requires frequent administration. Polymeric nanoparticles of this hydrophilic drug (RM-NPs) were developed to enhance its systemic concentration and BBB crossing capacity and characterized for particle size, zeta potential; entrapment efficiency. Ex-vivo permeation study was conducted to analyze solvent-system for increased permeation of RM across biological membrane which revealed RM showed maximum flux (96.66 ± 4.63 µg/cm²/h) at 8.36 ± 0.39h with 33% propylene glycol–ethanol while RM-NPs in distilled water showed 94.16 ± 3.62 µg/cm²/h flux at 6.80 ± 0.31h indicating that 33% propylene glycol–ethanol can serve as solvent-of-choice for transdermal delivery of rasagiline.

Graphical Abstract

Keywords:

• Binary solvent system
• biological membrane
• nanoparticles
• rasagiline mesylate
• transdermal permeation

Ethics statement

The animal study protocol was recommended and approved by the Institutional Animal Ethics Committee of University Department of Pharmaceutical Sciences, R. T. M. Nagpur University, Nagpur (Approval no. IAEC/UDPS/2017/14).

Acknowledgements

The Authors acknowledges the financial support from Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur under the scheme of U.R.P.S. (University Research Promotion Scheme). Authors wish to thank the Apotex Research Pvt. Ltd., Bangalore, India for proving gratis sample of rasagiline mesylate and also wish to thank Carbion Inc., Netherlands for providing gift sample of PLGA.

Disclosure statement

No potential conflict of interest was reported by the authors

Additional information

Funding

This work has been funded by Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur under the scheme of U.R.P.S. (University Research Promotion Scheme), Dev/RTMNURP/AH/1672.