Nano-ropinirole for the management of Parkinsonism: blood–brain pharmacokinetics and carrier localization

Mustafa, Gulam; Ahuja, Alka; Rohaimi, Abdulmohsen H. Al; Muslim, Shahnawaz; Hassan, Allam A.; Baboota, Sanjula; Ali, Javed

doi:10.1586/14737175.2015.1036743

Cited by 39 publications

(14 citation statements)

References 48 publications

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“…In what concerns the oral and oromucosal routes, the limitations are related with altered physiological states of individuals (such as nausea and vomiting, or the hypersalivation and inability to swallow that happen during an epileptic seizure) [3,4,[9][10][11], large intersubject absorption rate variability, slow onset of action, drug-drug and drug-food interactions and cytochrome P450 induction [8,10,[12][13][14][15][16][17]. Moreover, IN delivery offers the possibility of avoiding hepatic first pass metabolism and can reduce drug distribution to non-targeted sites, thereby minimizing systemic adverse effects [8,[18][19][20][21][22][23][24].…”

Section: Fig 1 Schematic Representation Of Intranasal (In) Deliverymentioning

confidence: 99%

Nanosystems in nose-to-brain drug delivery: A review of non-clinical brain targeting studies

Pires

Santos

2018

Journal of Controlled Release

152

133

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The treatment of neurodegenerative and psychiatric disorders remains a challenge in medical research. Several strategies have been developed over the years, either to overcome the blood-brain barrier or to achieve a safer or faster brain delivery, one of them being intranasal (IN) administration. The possibility of direct nose-to-brain transport offers enhanced targeting and reduced systemic side effects. Nevertheless, labile, low soluble, low permeant and/or less potent drugs might need a formulation other than the common solutions or suspensions. For that, the formulation of nanosystems is considered to be a promising approach, since it can protect drugs from chemical and/or metabolic degradation, enhance their solubility, or offer transport through biological membranes. However, the understanding of the factors promoting efficient brain targeting when using nanosystems through the nasal route is currently patchy and incomplete. The main purpose of the present review was to evaluate the association between brain delivery efficacy (in terms of brain targeting, brain bioavailability and time to reach the brain) and nanosystem type. For that, we performed a systematic bibliographic search and analysis. Furthermore, study designs, nanosystem properties, and reporting quality were also analyzed and discussed. It was found a high heterogeneity in how pre-clinical brain targeting studies have been conducted, analyzed and reported in scientific literature, which surely originates a significant degree of bias and data dispersion. This review attempts to provide some systematization recommendations, which may be useful for researchers entering the field, and assist in increasing the uniformity of future reports. The analysis of literature data confirmed that there is evidence of the advantage of the IN route (when compared to the intravenous route) and in using carrier nanosystems (when compared to IN solutions) for brain delivery of a large set of drugs. Among the most represented nanosystem classes, microemulsions had some of the lowest pharmacokinetic ratios values, while polymeric micelles had some of the best. Nevertheless, brain targeting efficacy comparisons between nanosystem groups had little statistical significance, and the superiority of the polymeric micelles group disappeared when nanosystems were compared to the respective IN drug solutions. In fact, some drugs reached the brain so efficiently, even as drug solutions, that further benefit from formulating them into nanosystems became less evident.

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Section: Fig 1 Schematic Representation Of Intranasal (In) Deliverymentioning

confidence: 99%

Nanosystems in nose-to-brain drug delivery: A review of non-clinical brain targeting studies

Pires

Santos

2018

Journal of Controlled Release

152

133

View full text Add to dashboard Cite

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“…Several studies have reported that the intranasal route can be a good option as a nose to brain targeting approach for treating the depressive disorders. ,− Trigeminal and olfactory pathways have been considered to be merely the routes via which the brain is linked to the outside environment [ , ]. Drugs with limited oral bioavailability because of substantial metabolism have been studied using this route as a viable alternative. − Additionally, the utilization of this nasal route of administration of medication allows the various therapeutics to avoid the first-pass effect. So, intranasal doses are frequently considered to be 2 to 10 times lower than doses that are administered orally .…”

Section: Discussionmentioning

confidence: 99%

Formulation, Characterization, and Evaluation of β-Cyclodextrin Functionalized Hypericin Loaded Nanocarriers

Waqar,

Zaman,

Hameed

et al. 2023

ACS Omega

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St. John's wort in western Europe has been extensively utilized for the treatment of mild to moderate depression. Hypericin, a red pigment, is found to be responsible for its antidepressant activity. The aim of the current study was to prepare a nanoemulsion (O/W) of hypericin designed for immediate delivery of the drug to the brain for the treatment of depression. The nanoemulsion was prepared by means of a homogenization technique, and that was followed by its physicochemical evaluation. Tween-80, Span-80, βcyclodextrin, ethanol, and eucalyptus oil were utilized for the manufacturing of the nanoemulsion. Morphological studies have revealed globular structures of nanosize that were confirmed by the zeta analysis. The consistency of particles was revealed by the low polydispersity values. pH values of all formulations lay within the range of nasal pH. The viscosity of the prepared formulations was affected by the increase in concentrations of β-cyclodextrin. After passing from the centrifugation and freeze−thaw studies, the prepared formulations showed good stability. Formulation F2 having a composition of oil phase (0.125 mL), aqueous phase (1.25 mL), and β-cyclodextrin (8%) showed the best results out of all the formulations, and F2 had a pH of 5.7, 5.35 cP viscosity, 1.332 refractive index, 148.8 globule size, and −10.8 zeta potential. The mean percentage drug release and in vitro and ex vivo percentage drug permeations were observed to be 71.75, 76, and 75.07%, respectively. Meanwhile, formulation F2 showed the maximum drug release and permeation. In vivo behavior studies including the open field test, elevated plus maze test, and tail suspension test were conducted to see the antidepressant effect of hypericin along with comparison with a commercially available treatment. In conclusion, the prepared formulation shows good efficacy as an antidepressant and can be considered as a natural alternative over synthetic drugs.

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“…The qualitative localization of florescent labelled PLGA NPs was determined in brain tissues by confocal laser microscopy (Olympus Fluoview™, Melville, NY, USA) [ 25 , 26 ]. For preparation of DAPI (4-6-diamidino-2-phenylindole) loaded PLGA nanoparticles, 0.2 mL of DAPI solution (50 μ g/mL in ethanol) was dissolved in PLGA solution and nanoparticles were prepared in similar way as described earlier.…”

Section: Methodsmentioning

confidence: 99%

Evaluation of Neuroprotective Effect of Thymoquinone Nanoformulation in the Rodent Cerebral Ischemia-Reperfusion Model

Xiao

Zhu

et al. 2016

BioMed Research International

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The purpose of the present study was to evaluate the neuroprotective efficacy of optimized thymoquinone loaded PLGA-chitosan nanoparticles delivered via nose to brain route in the rodent cerebral ischemia-reperfusion model. The neuroprotective efficacy of the optimized thymoquinone loaded PLGA-chitosan nanoparticles was evaluated in middle cerebral artery occluded rats by various pharmacodynamic and biochemical studies. The pharmacokinetics of thymoquinone loaded PLGA-chitosan nanoparticles in the brain and blood plasma together with qualitative localization of florescent labelled PLGA-chitosan nanoparticles in brain tissues were also determined. Intranasal delivery of optimized thymoquinone loaded PLGA-chitosan nanoparticles (183.5 ± 8.2 nm, 33.63 ± 2.25 mV) to brain significantly reduced the ischemia infarct volume and enhanced the locomotor activity and grip strength in the middle cerebral artery occluded rats. Biochemical studies showed that intranasal delivery of thymoquinone loaded PLGA-chitosan nanoparticles significantly reduced the lipid peroxidation but elevated the glutathione, catalase, and superoxide dismutase in the brain of middle cerebral artery occluded rats. The pharmacokinetic and localization studies showed that thymoquinone loaded PLGA-chitosan nanoparticles facilitated the delivery of thymoquinone to brain by intranasal nose to brain transport pathways and enhanced their pharmacokinetic profile in brain tissues. Thus, intranasal delivery of thymoquinone loaded PLGA-chitosan nanoparticles to brain could be potentially used for the neuroprotection and treatment of cerebral ischemia.

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Nano-ropinirole for the management of Parkinsonism: blood–brain pharmacokinetics and carrier localization

Abstract: Finally, the investigation demonstrated that intranasal delivery of mucoadhesive nanocarrier might play as a potential candidate in the management of Parkinson's disease and related brain disorders.

Cited by 39 publications

References 48 publications

Nanosystems in nose-to-brain drug delivery: A review of non-clinical brain targeting studies

Nanosystems in nose-to-brain drug delivery: A review of non-clinical brain targeting studies

Formulation, Characterization, and Evaluation of β-Cyclodextrin Functionalized Hypericin Loaded Nanocarriers

Evaluation of Neuroprotective Effect of Thymoquinone Nanoformulation in the Rodent Cerebral Ischemia-Reperfusion Model

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