Niosomes for nose-to-brain delivery of bromocriptine: Formulation development, efficacy evaluation and toxicity profiling

Sita, V G; Jadhav, Dhananjay; Vavia, Pradeep R.

doi:10.1016/j.jddst.2020.101791

Cited by 30 publications

(15 citation statements)

References 41 publications

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“…These results confirm previous reports of the cataleptic effect of haloperidol lasting for at least 120 min after administration ( Greco et al, 2010 ), being able to last up to 240–300 min after administration ( Verhagen-Kamerbeek et al, 1993 ; Moo-Puc et al, 2003 ; Ardashov et al, 2011 ; Ionov and Severtsev, 2012 ; Pavlova et al, 2014 ). The vehicle-treated group did not exhibit catalepsy over time, which is in agreement with evidence in the literature ( Colombo et al, 2013 ; Barroca et al, 2019 ; Sita et al, 2020 ), and attests that catalepsy is not predominant in the behavioral repertoire of rats even after multiple exposures to the test. Since catalepsy was successfully achieved with haloperidol 1 mg/kg for the entire period of testing, and this dose is widely used in the literature ( Waku et al, 2021 ), we considered haloperidol 1 mg/kg-induced catalepsy sufficient to assess the effects of aversive stimuli for the following experiments.…”

Section: Discussionsupporting

confidence: 91%

Effects of Immediate Aversive Stimulation on Haloperidol-Induced Catalepsy in Rats

Waku

Reimer

Oliveira

2022

Front. Behav. Neurosci.

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In animal models, the administration of the dopaminergic D2 antagonist haloperidol affects the nigrostriatal pathway, inducing catalepsy, a state of immobility similar to Parkinson’s disease (PD) bradykinesia and akinesia. In PD, the motor impairments are due to difficulties in selecting and executing motor actions, associated with dopamine loss in basal ganglia and cortical targets. Motor and affective limbic networks seem to be integrated via a striato-nigro-striatal network, therefore, it is not surprising that the motor impairments in PD can be influenced by the patient’s emotional state. Indeed, when exposed to aversive stimuli or life-threatening events, immobile patients are capable of performing sudden movements, a phenomenon known as paradoxical kinesia. Thus, the present study investigated the effects of unconditioned and conditioned aversive stimulation on haloperidol-induced catalepsy in rats. First, male Wistar rats received intraperitoneal administration of saline or haloperidol (1 or 2 mg/kg) and were evaluated in the catalepsy bar test to assess the cataleptic state induced by the different doses of haloperidol over time. Next, we evaluated the effects of two types of unconditioned aversive stimuli–100 lux light (1 and 20 s) or 0.6 mA footshock (1 s)–on the catalepsy. Finally, we evaluated the effects of light conditioned stimuli (Light-CS), previously paired with footshocks, on the cataleptic state. Catalepsy was observed following haloperidol 1 and 2 mg/kg administration. Exposure to footshocks, but not to light, significantly reduced step-down latency during the catalepsy test. Although unconditioned light did not affect catalepsy, paired Light-CS did reduce step-down latency. Here, we have provided evidence of face validity for the study of paradoxical kinesia. In addition to demonstrating that immediate exposure to an aversive stimulus is capable of disrupting the cataleptic state, our findings show that haloperidol-induced catalepsy seems to be differently influenced depending on the modality of aversive stimulation. Our data suggest that the selective recruitment of threat response systems may bypass the dysfunctional motor circuit leading to the activation of alternative routes to drive movement.

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Section: Discussionsupporting

confidence: 91%

Effects of Immediate Aversive Stimulation on Haloperidol-Induced Catalepsy in Rats

Waku

Reimer

Oliveira

2022

Front. Behav. Neurosci.

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“…The variation in publications per year is important data. As noted, the haloperidol‐induced catalepsy model for parkinsonism was first applied in the early 1980s (Chiu et al., 1981; Pycock et al., 1982; Schallert & Teitelbaum, 1981; Scheel‐Krüger & Magelund, 1981) and is still widely used nowadays (Bhattamisra et al., 2020; Chaudhary & Dhande, 2020; Kabra et al., 2020; Łażewska et al., 2020; Olaya et al., 2020; Parambi et al., 2020; Pardo et al., 2020; Sanawar et al., 2020; Sharma et al., 2020; Sita et al., 2020). In fact, since 2000, the number of articles published using this model has increased and become more constant (Figure 2).…”

Section: Discussionmentioning

confidence: 99%

Haloperidol‐induced catalepsy as an animal model for parkinsonism: A systematic review of experimental studies

Waku

Magalhães

Alves

et al. 2021

Eur J of Neuroscience

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Several useful animal models for parkinsonism have been developed so far. Haloperidol‐induced catalepsy is often used as a rodent model for the study of motor impairments observed in Parkinson's disease and related disorders and for the screening of potential antiparkinsonian compounds. The objective of this systematic review is to identify publications that used the haloperidol‐induced catalepsy model for parkinsonism and to explore the methodological characteristics and the main questions addressed in these studies. A careful systematic search of the literature was carried out by accessing articles in three different databases: Web of Science, PubMed and SCOPUS. The selection and inclusion of studies were performed based on the abstract and, subsequently, on full‐text analysis. Data extraction included the objective of the study, study design and outcome of interest. Two hundred and fifty‐five articles were included in the review. Publication years ranged from 1981 to 2020. Most studies used the model to explore the effects of potential treatments for parkinsonism. Although the methodological characteristics used are quite varied, most studies used Wistar rats as experimental subjects. The most frequent dose of haloperidol used was 1.0 mg/kg, and the horizontal bar test was the most used to assess catalepsy. The data presented here provide a framework for an evidence‐based approach to the design of preclinical research on parkinsonism using the haloperidol‐induced catalepsy model. This model has been used routinely and successfully and is likely to continue to play a critical role in the ongoing search for the next generation of therapeutic interventions for parkinsonism.

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“…Another research was designed to formulate nonionic surfactant vesicles loaded with Bromocriptine Mesylate (BCM) to enhance brain absorption via the nose-to-brain route. Compared to the BCM pharmaceutical solution, penetration through nasal mucosa was found to be elevated up to 6.4 times over the conventional drug solution in a 24-hour ex vivo study [36].…”

Section: Applications Of Niosomes-based Nasal Drug Delivery Systemsmentioning

confidence: 87%

“…Niosomes, which are prepared by following the same procedures and under the same variety of conditions, are structurally analogous to liposomes [35]. Besides, niosomes have several advantages over liposomes such as the ability to target the brain via using Receptor Facilitated Transcytosis (RFT), lower cost, scaling-up, and ease of formulation [36].…”

Section: Applications Of Niosomes-based Nasal Drug Delivery Systemsmentioning

confidence: 99%

Focus on Niosomal–based Drug Delivery Systems for Nasal Route: Applications and Challenges

Al-Zuhairy

El-Sawy²,

El-Nabarawi³

et al. 2023

Int J App Pharm

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For decades, the nasal route of administration is principally used for many therapeutic applications owing to the non-invasive nature of the nasal pathway. Besides, it circumvents blood-brain-barrier (BBB) and hepatic first-pass effect. Consequently, the nasal route is much preferred over other invasive approaches like intravenous, intracerebral, and transcranial for the systemic delivery of drugs and the treatment of central nervous systems (CNS) disorders such as depression, Alzheimer’s disease (AD), multiple sclerosis, and Parkinson’s disease (PD) via the nose-to-brain pathway. Drug applied via the nasal route displays some difficulty to reach the brain, like the dose limitation of the nasal pathway, mucociliary clearance, etc. The efficiency of the nasal route depends on the application delivery system. Lipidic-based drug delivery systems (liposomes, solid lipid nanoparticles …etc.) have been confirmed for their promising impact on the nasal delivery approach. Furthermore, the sensitivity of the nasal route and the touched-complications of clinical trials in CNS disorders assigns the necessity of consideration to the clinical trials and approval process of the niosomal-based nasal drug delivery approach. This review describes different approaches to nasal delivery, lipidic-based delivery systems with a focus on niosomes as a promising nasal delivery system, along with different formulation methodologies, and applications.

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Niosomes for nose-to-brain delivery of bromocriptine: Formulation development, efficacy evaluation and toxicity profiling

Cited by 30 publications

References 41 publications

Effects of Immediate Aversive Stimulation on Haloperidol-Induced Catalepsy in Rats

Effects of Immediate Aversive Stimulation on Haloperidol-Induced Catalepsy in Rats

Haloperidol‐induced catalepsy as an animal model for parkinsonism: A systematic review of experimental studies

Focus on Niosomal–based Drug Delivery Systems for Nasal Route: Applications and Challenges

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