Therapeutic Approaches for the Management of Parkinson's Disease

Prasad, Jhakeshwar; Netam, Ashish Kumar; Singh, Ravinder; Sahu, Manisha; Satapathy, Trilochan; Rao, S. Prakash; Baghel, Purnima; Sahu, Mahendra

doi:10.5958/2321-5836.2019.00009.0

Cited by 3 publications

(1 citation statement)

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“…The significant pathological change in patients with PD is the loss of melanin-containing dopaminergic neurons in the zona compacta of the substantia nigra 4 . These pigmented neurons have been identified as nigrostriatal dopamine neurons; loss of these neurons results in a decrease of dopamine content in the striatum 5 .…”

Section: Introductionmentioning

confidence: 99%

Preparation, In Vitro characterization and stability studies of ropinirole lipid nanoparticles enriched hydrogel for treatment of neurodegeneration diseases

Samanthula¹,

Alli²,

Gorre³

2021

J. Drug Delivery Ther.

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Ropinirole (RP), is a selective dopamine agonist that is used alone or with other medications to treat the symptoms of Parkinson’s disease (PD). RP has low bioavailability of only about 50% due to the first-pass metabolism, and it requires frequent dosing during oral administration. The objective of the current research was to develop RP loaded solid lipid nanoparticles (RP-SLNs), nanostructured lipid carriers (RP-NLCs), and their corresponding hydrogels (RP-SLN-C and RP-NLC-C) that might improve efficacy in PD treatment. RP nanoparticles were prepared by homogenization aided probe sonication method and optimized based on particle size, polydispersity index (PDI), zeta potential (ZP), assay, entrapment efficiency, and in vitro release studies. Optimized formulations were converted to hydrogel formulations using Carbopol 934 as a gelling polymer and optimized based on rheological and release characteristics. Optimized formulations were further evaluated using differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD), scanning electron microscopy (SEM), freeze-drying, and stability study at refrigerated and room temperatures. The optimized RP-SLN formulation showed particle size and entrapment efficiency of 213.5±3.8 nm and 77.9±3.1% compared to 190.6±3.7 nm and 85.7±1.7% for optimized RP-NLC formulation. PXRD supplemented and confirmed DSC results, RP was entrapped in a molecularly dispersed state inside the core of the lipid nanocarrier. Furthermore, RP loaded lipid nanocarriers revealed a spherical shape in SEM images. In vitro release studies demonstrated sustained release profiles for RP from SLNs, NLCs, and their hydrogels over 24 h and were stable over three months at 4ºC and 25ºC storage conditions. Keywords: Parkinson’s disease, Ropinirole, Solid lipid nanoparticles, Nanostructured lipid carriers, Hydrogel.

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Section: Introductionmentioning

confidence: 99%

Preparation, In Vitro characterization and stability studies of ropinirole lipid nanoparticles enriched hydrogel for treatment of neurodegeneration diseases

Samanthula¹,

Alli²,

Gorre³

2021

J. Drug Delivery Ther.

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Therapeutic effect of Embelin and Levodopa combination in Rotenone induced Parkinson’s disease in mice on Neurobehavioral Changes

Koppal,

H. R,

Sivanesan

et al. 2023

RJPT

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Objective: The present work evaluated the therapeutic potential of embelin monotherapy, embelin plus levodopa (L-Dopa) combination therapy in rotenone induced Parkinson’s disease (PD) model mice. Scope: Based on several growing evidence, antioxidants can be considered as modifiable factors that eventually decrease the risk of degeneration and progression of PD. Especially anti-oxidants from herbal medicines play vital role against several degenerative diseases. Therefore, we evaluated the neuroprotective effect of embelin and embelin plus L-Dopa therapy in rotenone induced behavioural changes in mice. Methods: Swiss Albino male adult mice were randomly divided into 7 groups. Group-1 (Control) 2mL/kg olive oil by oral route (p.o.), Groups from 2 to 7 were induced with 2.5mg/kg rotenone by intraperitoneal route (i.p.), L-Dopa 7.5mg/kg p.o was administered to Group-3. Group-4 and Group-5 were given 20mg/kg and 40mg/kg embelin p.o. Group 6 and 7 were given embelin p.o. at a dose of 20mg and 40mg/kg respectively along with 7.5mg/kg L-Dopa p.o. Result: Administration of rotenone (2.5mg/kg) for twenty-one days to mice consecutively produced motor incoordination, decreased locomotor activity anxiety like behaviours and bradykinesia. Embelin monotherapy as well as combination therapy of embelin along with L-Dopa significantly decreased the effect of rotenone on behavioural changes and rendered neuroprotection in a dose dependant manner.

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Calpain: An Emerging Therapeutic Target

Prajapati,

Singh

2024

RJPPD

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Calpain was first found in the year 1964 as a calcium associated cysteine protease enzyme. Mostly, it is present in all the eukaryotes and other organism. Despite of being an enzyme calpain is involved in cellular organization rather than proteolytic digestion. For calpain activation, adequate concentration of calcium is required. Rest of the concentration they get from endoplasmic reticulum (ER), calcium influx during oxidative stress etc. In adverse condition calpain utilized all the excess calcium and activates molecular cascade involved in progression of various disease. Pathogenesis of every disease is highly protein specific such as in Alzheimer’s disease CDK5 and MAPK, phosphorylate Tau proteins in the brain. Further, Beclin 1, Bcl 2 and PGC-1α interfere with the mitochondrial function in heart resulting in abnormal functioning. Few studies have been suggesteddeactivation of calpain may ameliorate pathological conditions but still there are certain checkpoints which are still unexplored and need attention. Calpain has role in several pathological conditions but in this comprehensive review, we expect to cover how calpain is involved in the pathogenesis of neurodegenerative disorders, cardiovascular and cancer. This review also explained findings of different researchers on use of calpain inhibitors and impact of knocking down calpain gene in amelioration of pathogenesis. This advanced knowledge of mechanismand findings would be helpful for further development of calpain inhibitors for clinical use.

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Therapeutic Approaches for the Management of Parkinson's Disease

Cited by 3 publications

References 0 publications

Preparation, In Vitro characterization and stability studies of ropinirole lipid nanoparticles enriched hydrogel for treatment of neurodegeneration diseases

Preparation, In Vitro characterization and stability studies of ropinirole lipid nanoparticles enriched hydrogel for treatment of neurodegeneration diseases

Therapeutic effect of Embelin and Levodopa combination in Rotenone induced Parkinson’s disease in mice on Neurobehavioral Changes

Calpain: An Emerging Therapeutic Target

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