Impact of rasagiline nanoparticles on brain targeting efficiency via gellan gum based transdermal patch: A nanotheranostic perspective for Parkinsonism.
Administration, Cutaneous
Administration, Oral
Animals
Behavior, Animal
Brain
/ drug effects
Catalepsy
Diffusion
Indans
/ pharmacology
Kinetics
Male
Nanoparticles
Parkinsonian Disorders
/ drug therapy
Particle Size
Polyesters
/ chemistry
Polysaccharides, Bacterial
/ chemistry
Rats
Rats, Wistar
Skin
/ drug effects
Solvents
Tensile Strength
Theranostic Nanomedicine
Tissue Distribution
Transdermal Patch
Brain targeting
Gellan gum
In-vivo anti-Parkinson study
In-vivo imaging
Rasagiline nanoparticles
Transdermal film
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
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
1006-1024Informations 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.