Impact of rasagiline nanoparticles on brain targeting efficiency via gellan gum based transdermal patch: A nanotheranostic perspective for Parkinsonism.


Journal

International journal of biological macromolecules
ISSN: 1879-0003
Titre abrégé: Int J Biol Macromol
Pays: Netherlands
ID NLM: 7909578

Informations de publication

Date de publication:
01 Dec 2020
Historique:
received: 03 03 2020
revised: 24 06 2020
accepted: 26 06 2020
pubmed: 4 7 2020
medline: 7 4 2021
entrez: 4 7 2020
Statut: ppublish

Résumé

Rasagiline mesylate is used as first line agent for early management of Parkinson's disease but its water soluble nature creates hurdles to cross blood brain barrier also its low oral bioavailability and rapid elimination requires frequent dosing. Thus present study aims to prepare rasagiline mesylate-nanoparticles (RM-NPs) loaded gellan gum transdermal film for non-invasive; self-administration in elderly patients. PLGA coated RM-NPs prepared by solvent evaporation technique were incorporated into film prepared by solvent casting method. Optimized films with 1.127 g gellan gum and 1.962 % linoleic acid showed enhanced ex-vivo diffusion over a period of 72 h. Comparative pharmacokinetic study revealed increased bioavailability of rasagiline on transdermal application compared to oral route. In-vivo anti-Parkinson activity estimated by behavioural and biochemical analysis indicate reserpine to interfere with monoamine storage hence resulting in development of akinesia and PD-like symptoms in rats. Brain targeting monitored by gamma imaging showed effective brain drug uptake from transdermal film which was also supported by increased brain targeting efficiency estimated from biodistribution study. Thus, the data support efficacy of gellan gum film to target drug to brain region compared to oral route and hence can be employed as a convenient approach for long-term treatment of Parkinson's disease in elderly patients.

Identifiants

pubmed: 32619667
pii: S0141-8130(20)33708-9
doi: 10.1016/j.ijbiomac.2020.06.261
pii:
doi:

Substances chimiques

Indans 0
Polyesters 0
Polysaccharides, Bacterial 0
Solvents 0
rasagiline 003N66TS6T
poly(lactide) 459TN2L5F5
gellan gum 7593U09I4D

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

1006-1024

Informations de copyright

Copyright © 2020 Elsevier B.V. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of competing interest The authors have no competing interests to declare.

Auteurs

Nikhil R Bali (NR)

University Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur 440 033, Maharashtra, India. Electronic address: nikhilbali@outlook.com.

Pramod S Salve (PS)

University Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur 440 033, Maharashtra, India.

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Classifications MeSH