Solid lipid nanoparticles for nose to brain delivery of haloperidol: in vitro drug release and pharmacokinetics evaluation

Yasir, Mohd; Sara, Udai Vir Singh

doi:10.1016/j.apsb.2014.10.005

Cited by 130 publications

(67 citation statements)

References 43 publications

(50 reference statements)

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“…The samples were injected using a 20 μL HPLC injector. All determinations were performed at ambient temperature for a run time of 5 min [22].…”

Section: Hplc Methodsmentioning

confidence: 99%

Development and Validation of a New HPLC Method for In-vitro Studies of Haloperidol in Solid Lipid Nanoparticles

Yasir¹,

Sara²,

Som³

et al. 2016

J Anal Bioanal Tech

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A simple and sensitive HPLC method was developed and validated for the study of in-vitro drug release from haloperidol loaded solid lipid nanoparticles (SLNs). The method was also used for the analysis of drug for detection of shelf life of developed SLNs. 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 1-60 µg/mL. The value of LOD and LOQ was found to be 0.045 and 0.135 μg/ml respectively. The drug loaded SLNs showed sustained drug release with maximum value of 95.52 ± 5.21% in 24 h. The shelf life of SLNs formulation was found to be 2.31 years at 4°C.

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“…The samples were injected using a 20 μL HPLC injector. All determinations were performed at ambient temperature for a run time of 5 min [22].…”

Section: Hplc Methodsmentioning

confidence: 99%

Development and Validation of a New HPLC Method for In-vitro Studies of Haloperidol in Solid Lipid Nanoparticles

Yasir¹,

Sara²,

Som³

et al. 2016

J Anal Bioanal Tech

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“…IR spectra of Zolmitriptan and physical mixture of Zolmitriptan, HPMC E-15, Lycoat (1:1) were scanned from 4000 cm −1 to 500 cm −1 and interpreted. [11] Preparation of Zolmitriptan loaded fast disintegrating oral film Solvent casting method was employed to formulate oral films. [12] [13] Various placebo films were prepared using varied combinations of hydrophilic polymers by trial and error method.…”

Section: Drug-excipients Compatibility Studymentioning

confidence: 99%

Oral Delivery of Zolmitriptan Loaded Fast Disintegrating Film: Formulation Development, Statistical Optimization, in-Vitro and in-Vivo Evaluation

Chauhan¹,

Yasir

Verma³

2019

J App Pharm Sci Res

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Introduction:Fast dissolving film technology has been developed out as a alternative drug delivery system that gives an exception advantage for taking medications. Objective: The aim of this study was to formulate and evaluate the Zolmitriptan loaded fast disintegrating oral film by solvent casting method. Material and methods: A preliminary study was conducted to select a suitable film forming polymer and plasticiser concentration.The formulation was optimized with the help of 2 2 factorial designs in which polymer and plasticizer concentration at two levels was taken as independent factors and disintegration time, tensile strength and % elongation were taken as dependent factors. The optimized formulation OP1 was subjected to stability study as per the ICH guidelines at 40 ± 0.5 0 C / 75 ± 5% RH for six months. In vivo studies were conducted on Wister albino rats and concentration of drug in blood was analysed by HPLC technique. Various pharmacokinetic parameters for OP1 were determined and compared with reference formulation (drug sol.). Result and Discussion: For optimized formulation various parameters were found to be in acceptable range and it was stable under specified conditions. The value of AUC0-t (ng h/ml), AUC0-∞ (ng h/ml) of the OP1 was found to be 723.91± 84.21, 770.90 ± 104.32, respectively, for the drug sol 468.56 ± 79.36, 500.37 ± 95.43 respectively. Relative bioavailability of OP1 was 1.55 time than that of drug sol. Conclusion: The formulation not only increases the bioavailability of drug but also produce the quick action for the migraine patients.

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“…Dose for the rats was calculated taking into consideration ratio of surface area of a rat to that of a human being (Yasir, Sara, 2014b). Surface area ratio for a rat (200 g) to a human (70 kg) is 56.…”

Section: Calculation Of Dose For Ratsmentioning

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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Solid lipid nanoparticles for nose to brain delivery of haloperidol: in vitro drug release and pharmacokinetics evaluation

Cited by 130 publications

References 43 publications

Development and Validation of a New HPLC Method for In-vitro Studies of Haloperidol in Solid Lipid Nanoparticles

Development and Validation of a New HPLC Method for In-vitro Studies of Haloperidol in Solid Lipid Nanoparticles

Oral Delivery of Zolmitriptan Loaded Fast Disintegrating Film: Formulation Development, Statistical Optimization, in-Vitro and in-Vivo Evaluation

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

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