Intranasal nanoemulsion based brain targeting drug delivery system of risperidone

Kumar, Mrityunjay; Misra, Ambikanandan; Babbar, Anil Kumar; Mishra, Anil K.; Mishra, Pravakar; Pathak, Kamla

doi:10.1016/j.ijpharm.2008.03.029

Cited by 384 publications

(185 citation statements)

References 25 publications

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“…The mice were held from the back in slanted position and were placed in supine position with head angle at 0 (horizontal) during administration as well as were held for approximately 2 min after administration of doses. The mice were anaesthetised with 10% chloral hydrate solution and sacrificed humanely by cervical dislocation method at different time intervals (0.5, 1, 2, 4 and 8 h) and the blood was collected using cardiac puncture [28]. The collected blood was mixed properly with the anticoagulant and centrifuged at 1000 Â g for 10 min.…”

Section: Brain and Blood Distribution Of Brc-loaded Cs Npsmentioning

confidence: 99%

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: Brain and Blood Distribution Of Brc-loaded Cs Npsmentioning

confidence: 99%

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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“…The small globule size and low polydispersity indices (0.217 ± 0.051 to 0.243 ± 0.03) for MEs indicated large surface area with the potential of high drug permeability. Stability was confirmed by the negative zeta potential (Vyas et al, 2005(Vyas et al, , 2006bKumar et al 2008aKumar et al , 2008b. The pH of all the ME formulations was found to be in range of 5.4-5.5 and considered suitable for intranasal (Washington et al, 2000) and intravenous administration.…”

Section: Drug-loaded Microemulsionsmentioning

confidence: 91%

Docosahexaenoic acid–mediated, targeted and sustained brain delivery of curcumin microemulsion

Shinde

Devarajan

2017

Drug Delivery

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We disclose microemulsions (ME) of curcumin (CUR) with docosahexaenoic acid (DHA)-rich oil (CUR DHA ME) for targeted delivery to the brain. MEs of CUR (5 mg/mL) with and without DHArich oil (CUR Capmul ME) suitable for intravenous and intranasal administration exhibited negative zeta potential, globule size 520 nm and good stability. Following intravenous delivery MEs exhibited high brain concentration with CUR DHA ME exhibiting a 2.8-fold higher C max than CUR solution. Furthermore, high and sustained concentration was demonstrated even at 24 h, which was 8-and 2-fold higher than CUR solution and CUR Capmul ME, respectively. Brain concentrations following intranasal administration were, however, substantially higher as evident from higher C max and AUC and sustained compared to corresponding intravenous formulations signifying nose to brain targeting. The high brain concentration of CUR DHA ME is ascribed to the targeting efficiency enabled by DHA-mediated transport across the blood-brain barrier (BBB). Histopathological and nasal toxicity confirmed safety of the MEs. Concentrationdependent cytotoxicity in vitro, on human glioblastoma U-87MG cell line was observed with CUR DHA MEs and with the blank DHA ME, implying anticancer potential of DHA. The dramatically low IC 50 value of CUR DHA ME (3.755 ± 0.24 ng/mL) is therefore attributed to the synergistic effect of CUR and DHA in the ME. The CUR concentration achieved with CUR DHA ME at 24 h which translated to 466-fold(intranasal) and 421-fold (intravenous) the IC 50 value in the U-87MG cell line suggests great promise of CUR DHA ME for therapy of brain cancer by both routes.

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“…The blood was centrifuged at 4000 rpm for 20 min and aliquots of the supernatant separated and stored at -21 °C until drug analysis was carried out using HPLC (Kumar et al, 2008).…”

Section: Procedures For Blood Samplingmentioning

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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Intranasal nanoemulsion based brain targeting drug delivery system of risperidone

Cited by 384 publications

References 25 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

Docosahexaenoic acid–mediated, targeted and sustained brain delivery of curcumin microemulsion

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

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