Chitosan coated synergistically engineered nanoemulsion of Ropinirole and nigella oil in the management of Parkinson's disease: Formulation perspective and In vitro and In vivo assessment.
Animals
Benzoquinones
/ pharmacology
Chitosan
/ chemistry
Disease Models, Animal
Drug Stability
Drug Synergism
Emulsions
Female
Humans
Indoles
/ administration & dosage
Male
Molecular Docking Simulation
NF-kappa B
/ chemistry
Nanoparticles
Nigella
/ chemistry
Oxidopamine
/ adverse effects
Parkinson Disease
/ drug therapy
Plant Oils
/ administration & dosage
Rats
Tumor Necrosis Factor-alpha
/ chemistry
Mucoadhesion
Nanoemulsion
Neuroinflammation
Oxidative stress
Parkinson's disease
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:
15 Jan 2021
15 Jan 2021
Historique:
received:
23
06
2020
revised:
22
11
2020
accepted:
29
11
2020
pubmed:
6
12
2020
medline:
20
4
2021
entrez:
5
12
2020
Statut:
ppublish
Résumé
The research presented aims at developing Ropinirole hydrochloride (RHCl) nanoemulsion (NE) with nigella oil for Parkinson's disease (PD). In silico study was done to explore interactions of ropinirole and thymoquinone at receptor site (TNF-α and NFK-β). Ropinirole and Thymoquinone forms a hydrogen bond with residue Arginine 201 and residue Arginine 253 with a bond length of 1.89 Å and 2.30 Å at the NF-κβ receptor. NE was optimized using Central Composite Rotatable Design (CCRD). The globule size of chitosan coated NE, Polydispersity index (PDI) and zeta potential were 183.7 ± 5.2 nm, 0.263 ± 0.005, and 24.9 mV respectively. NE exhibited 85.28% transmittance showing the formulation was clear and transparent. TEM showed that NE had spherical globules with no aggregation. The formulation had a stable pH value of 5.8 ± 0.18. In vitro release and permeation studies exhibited 2 folds and 3.4 folds enhancement when compared with the drug suspension. Neurobehavioral activity and biochemical parameters corroborated well with the pharmacokinetic results. Histopathological study and immunohistochemical analysis were performed to get better picture of 6-OHDA induced toxicity and reversal of PD symptoms. Thus, the NE tailored is a promising synergistic approach yielding enticing outcomes for better management of PD related symptoms.
Identifiants
pubmed: 33278450
pii: S0141-8130(20)35145-X
doi: 10.1016/j.ijbiomac.2020.11.207
pii:
doi:
Substances chimiques
Benzoquinones
0
Emulsions
0
Indoles
0
NF-kappa B
0
Plant Oils
0
Tumor Necrosis Factor-alpha
0
ropinirole
030PYR8953
Oxidopamine
8HW4YBZ748
Chitosan
9012-76-4
thymoquinone
O60IE26NUF
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
605-619Informations de copyright
Copyright © 2020 Elsevier B.V. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest There is no conflict of interest between the authors.