Bromocriptine loaded chitosan nanoparticles intended for direct nose to brain delivery: Pharmacodynamic, Pharmacokinetic and Scintigraphy study in mice model

Shadab,; Khan, Rashid Ali; Mustafa, Gulam; Chuttani, Krishna; Baboota, Sanjula; Sahni, Jasjeet Kaur; Ali, Javed

doi:10.1016/j.ejps.2012.12.007

Cited by 236 publications

(126 citation statements)

References 36 publications

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“…The mean zeta potential of BRC-loaded CS NPs was found to be +40.32 ± 2.78 mV, which revealed that prepared formulations were stable [31]. The surface morphology of CS NPs recorded from SEM was either spherical or ellipsoidal with smooth surface (figure not shown) [15]. The percentage release profile of BRC from the nanoparticulate formulation was investigated in phosphate buffer solution (pH 7.4).…”

Section: Preparation and Characterisation Of Npsmentioning

confidence: 99%

“…When BRC-loaded CS NPs were administered intravenously, the C max (0.823 ± 0.099 ng/ml and 0.259 ± 0.081 ng/ml) was reached at 1 h in blood and brain. When BRC-loaded CS NPs was administered intravenously, higher quantity of BRC did not reach in brain because BRC-loaded CS NPs with their high positive surface was rapidly recognised by the reticuloendothelial system in blood [15]. A small quantity of BRC was detected in brain because some of the CS NPs may have crossed through BBB due to small size of NPs and presence of CS, which has also been proven to be an efficient absorption enhancer that can transiently open tight junctions between epithelial cells of BBB and thereby significantly enhance the absorption of BRC in brain [25].…”

Section: Optimised Nanoformulation Of Brc For Direct Nose-to-brain Dementioning

confidence: 99%

“…BRC has also been reported to have antioxidant effects, inhibit free radical formation and scavenge free radicals and retard apoptosis, which is probably accelerated in PD [14,15]. BRC is available in tablet and capsule dosage form (2.5 --20 mg/day, in divided doses), and these dosage forms exhibit low bioavailability (6%) due to extensive first-pass metabolism and non-targeted delivery results in side effects such as GI side effects, headache and dizziness [16].…”

Section: Introductionmentioning

confidence: 99%

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Optimised nanoformulation of bromocriptine for direct nose-to-brain delivery: biodistribution, pharmacokinetic and dopamine estimation by ultra-HPLC/mass spectrometry method

Shadab

Haque

Fazil

et al. 2014

Expert Opinion on Drug Delivery

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Section: Preparation and Characterisation Of Npsmentioning

confidence: 99%

Section: Optimised Nanoformulation Of Brc For Direct Nose-to-brain Dementioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Optimised nanoformulation of bromocriptine for direct nose-to-brain delivery: biodistribution, pharmacokinetic and dopamine estimation by ultra-HPLC/mass spectrometry method

Shadab

Haque

Fazil

et al. 2014

Expert Opinion on Drug Delivery

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“…Chitosan NP were developed for intranasal delivery of bromocriptine [27]. NP were characterized, presenting a size of 160 nm which is compatible with transcellular transport through olfactory neurons to the brain.…”

Section: Dds For Agonist Deliverymentioning

confidence: 99%

Drug development in Parkinson's disease: From emerging molecules to innovative drug delivery systems

2013

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Current treatments for Parkinson's disease (PD) are aimed at addressing motor symptoms but there is no therapy focused on modifying the course of the disease.Successful treatment strategies have been so far limited and brain drug delivery remains a major challenge that restricts its treatment. This review provides an overview of the most promising emerging agents in the field of PD drug discovery, discussing improvements that have been made in brain drug delivery for PD. It will be shown that new approaches able to extend the length of the treatment, to release the drug in a continuous manner or to cross the blood brain barrier and target a specific region are still needed.Overall, the results reviewed here show that there is an urgent need to develop both symptomatic and disease-modifying treatments, giving priority to neuroprotective treatments. Promising perspectives are being provided in this field by rasagiline and by neurotrophic factors like glial cell line-derived neurotrophic factor. The identification of disease-relevant genes has also encouraged the search for disease-modifying therapies that function by identifying molecularly-targeted drugs. The advent of new molecular and cellular targets like α-synuclein, leucine-rich repeat serine/threonine protein kinase 2 or parkin, among others, will require innovative delivery therapies. In this regard, drug delivery systems (DDS) have shown great potential for improving the efficacy of conventional and new PD therapy and reducing its side effects. The new DDS discussed here, which include microparticles, nanoparticles and hydrogels among others, will probably open up possibilities that extend beyond symptomatic relief. However, further work needs to be done before DDS become a therapeutic option for PD patients.

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“…The extent of nose-to-brain delivery could be evaluated by many parameters (Abdelbeary, Tadros, 2013): (i) The brain/blood ratio, at 0.5 h, following intranasal and intravenous administration (Vyas et al, 2005). (ii) The relative bioavailability (RB) percentages following the intranasal administration in the blood and brain (MD et al, 2012). (iii) The drug targeting index (DTI) (Wang, Jiang, Lu, 2003).…”

Section: Procedures Of Drug Extraction From Plasma By Liquidliquid Extmentioning

confidence: 99%

Development of a new HPLC method for in vitro and in vivo studies of haloperidol in solid lipid nanoparticles

Yasir

Sara²,

Som³

2017

Braz. J. Pharm. Sci.

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A simple and sensitive HPLC method was developed and validated for the quantification of haloperidol in solid lipid nanoparticles (SLNs). The developed method was used for detection of shelf life of haloperidol in SLNs. Calibration curve of haloperidol was also constructed in rat plasma using loratidine as internal standard. In vivo studies were performed on rats and concentration of haloperidol in brain and blood was measured for the determination of various pharmacokinetic and hence brain targeting parameters. Chromatogram separation was achieved using C18 column as stationary phase. The mobile phase consisted of 100 mM/L potassium dihydrogen phosphate-acetonitrile-TEA (10:90:0.1, v/v/v) and the pH was adjusted with o-phosphoric acid to 3.5. Flow rate of mobile phase was 2 mL/minute and eluents were monitored at 230 nm using UV/VIS detector. The method was validated for linearity, precision, accuracy, reproducibility, limit of detection (LOD) and limit of quantification (LOQ). Linearity for haloperidol was in the range of 1-16 µg/mL. The value of LOD and LOQ was found to be 0.045 and 0.135 μg/mL respectively. The shelf life of SLNs formulation was found to be 2.31 years at 4 o C. Various parameters like drug targeting index (DTI), drug targeting efficiency (DTE) and nose-to-brain direct transport (DTP) were determined for HP-SLNs & HP-Sol administered intranasally to evaluate the extent of nose-to-brain delivery. The value of DTI, DTE and DTP for HP-SLNs was found to be 23.62, 2362.43 % and 95.77% while for HP-Sol, values were 11.28, 1128.61 % and 91.14 % respectively.Uniterms: Haloperidol/quantification. Haloperidol/pharmacokinetic. Haloperidol/in vitro study. Haloperidol/in vivo study. High performance liquid chromatography/solid lipid nanoparticles. Plasma. Validation. Brain targeting.

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Bromocriptine loaded chitosan nanoparticles intended for direct nose to brain delivery: Pharmacodynamic, Pharmacokinetic and Scintigraphy study in mice model

Cited by 236 publications

References 36 publications

Optimised nanoformulation of bromocriptine for direct nose-to-brain delivery: biodistribution, pharmacokinetic and dopamine estimation by ultra-HPLC/mass spectrometry method

Optimised nanoformulation of bromocriptine for direct nose-to-brain delivery: biodistribution, pharmacokinetic and dopamine estimation by ultra-HPLC/mass spectrometry method

Drug development in Parkinson's disease: From emerging molecules to innovative drug delivery systems

Development of a new HPLC method for in vitro and in vivo studies of haloperidol in solid lipid nanoparticles

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