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

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 cro...

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Bibliographic Details
Published inInternational journal of polymeric materials Vol. 70; no. 3; pp. 158 - 173
Main Authors Bali, Nikhil R., Shinde, Mahesh P., Rathod, Shahadev B., Salve, Pramod S.
Format Journal Article
LanguageEnglish
Published Philadelphia Taylor & Francis 11.02.2021
Taylor & Francis Ltd
Subjects
Binary solvent system
Bioavailability
biological membrane
Design optimization
Distilled water
Entrapment
Ethanol
Membranes
Nanoparticles
Penetration
Propylene
rasagiline mesylate
Solvents
transdermal permeation
Zeta potential
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Summary: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/cm 2 /h) at 8.36 ± 0.39h with 33% propylene glycol-ethanol while RM-NPs in distilled water showed 94.16 ± 3.62 µg/cm 2 /h flux at 6.80 ± 0.31h indicating that 33% propylene glycol-ethanol can serve as solvent-of-choice for transdermal delivery of rasagiline.
ISSN:0091-4037
1563-535X
DOI:10.1080/00914037.2019.1706507