Distribution of liposomal breviscapine in brain following intravenous injection in rats

Lv, Wenli; Guo, Zhixiong; Li, Jin; Huang, Luosheng; Ping, Qineng

doi:10.1016/j.ijpharm.2005.09.012

Cited by 27 publications

(14 citation statements)

References 2 publications

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“…The analysis of breviscapine in plasma was performed using a Shimadzu HPLC system (Kyoto, Japan) and the UV detector equipped with a C18 analytical column (150 mm×4.6 mm, 5 μm). The mobile phase consisted of 0.2% phosphoric acid, acetonitrile and methanol (65/10/25, v/v/v) at a flow rate of 1.0 mL/min [23] . A processed plasma sample (20 μL) was injected into the analysis system.…”

Section: Analysis Methodsmentioning

confidence: 99%

Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Zheng

Shan

et al. 2013

Acta Pharmacol Sin

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Aim: Breviscapine isolated from the Chinese herb Erigeron breviscapus (Vant) Hand-Mazz is widely used to treat cardiovascular and cerebrovascular diseases. The aim of this study was to improve the pharmacokinetic profiles of breviscapine using nanostructured lipid carrier based on an ionic complex formation. Methods: Breviscapine nanostructured lipid carrier (Bre-NLC) was prepared using the thin film homogenization method. The morphology of Bre-NLCs was determined using transmission electron microscopy. The mean particle size, polydispersity index, zeta-potential analysis and entrapment efficiency were analized. In vitro release was studied using the dialysis method. In vitro stability was studied in fresh plasma and liver slurry of rats. In vivo pharmacokinetics was analyzed in rats after intravenous injection of a dose equivalent to breviscapine (10 mg/kg). Results: The Bre-NLCs were spherical with a mean particle size of ~170 nm, a zeta potential of ~20 mV and a high entrapment efficiency of ~89%. Compared with a commercially available solution, a substantial decrease in the cumulative release of breviscapine was found for the Bre-NLCs. The NLC has a significantly protective effect against the liver enzyme degradation of breviscapine. After intravenous administration in rats, the Bre-NLCs exhibited a 32 times increase in the AUC 0-t and a 12 times increase in T 1/2 as compared to the commercially available breviscapine solution. Conclusion:The results demonstrate that the NLC has great potential to use as a novel sustained release system for breviscapine.

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Section: Analysis Methodsmentioning

confidence: 99%

Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Zheng

Shan

et al. 2013

Acta Pharmacol Sin

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“…Breviscapine has several commercially produced preparations like tablets and injections available in the market and has been widely used in the clinic to treat acute cerebral infarction and paralysis induced by cerebrovascular diseases such as hypertension, cerebral thrombosis, and cerebral hemorrhage (2,3). However, like lots of other naturally extracted flavonoid drugs with proved pharmacological activities, the clinical application of breviscapine has been limited due to its poor physicochemical properties such as low aqueous solubility and poor chemical stability which results to a limited bioavailability with an absolute bioavailability of only 0.40± 0.19% reported for oral preparations (4,5). Adding to the poor physicochemical properties of breviscapine is the daunting challenge posed by the blood-brain barrier (BBB) in delivering the drug molecules into the brain.…”

Section: Introductionmentioning

confidence: 99%

“…Polymeric nanoparticles (9), liposomes (5), and nanosuspension (10) formulations of breviscapine have been reported with some successes. However, these reports have various limitations such as effects of the reticuloendothelial system (RES), possible toxicity in the case of degradation of polymeric materials, and less objective methods of in vivo evaluation which involved evaluation of brain tissues post-sacrifice of the animals.…”

Section: Introductionmentioning

confidence: 99%

Mixed Polyethylene Glycol-Modified Breviscapine-Loaded Solid Lipid Nanoparticles for Improved Brain Bioavailability: Preparation, Characterization, and In Vivo Cerebral Microdialysis Evaluation in Adult Sprague Dawley Rats

et al. 2014

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Abstract. Breviscapine is used in the treatment of ischemic cerebrovascular diseases, but it has a low bioavailability in the brain due to its poor physicochemical properties and the activity of P-glycoprotein efflux pumps located at the blood-brain barrier. In the present study, breviscapine-loaded solid lipid nanoparticles (SLN) coated with polyethylene glycol (PEG) derivatives were formulated and evaluated for their ability to enhance brain bioavailability. The SLNs were either coated with polyethylene glycol (40) (PEG-40) stearate alone (Bre-GBSLN-PS) or a mixture of PEG-40 stearate and 1,2-distearoyl-snglycero-3-phosphoethanolamine-N-PEG2000 (DSPE-PEG 2000 ) (Bre-GBSLN-PS-DSPE) and were characterized both in vitro and in vivo. The mean particle size, polydispersity index, and entrapment efficiency for Bre-GBSLN-PS and Bre-GBSLN-PS-DSPE were 21.60±0.10 and 22.60±0.70 nm, 0.27±0.01 and 0.26 ±0.04, and 46.89±0.73% and 47.62±1.86%, respectively. The brain pharmacokinetic parameters revealed that the brain bioavailability of breviscapine from the Bre-GBSLN-PS and Bre-GBSLN-PS-DSPE was significantly enhanced (p<0.01) with the area under concentration-time curve (AUC) of 1.59±0.39 and 1.42±0.58 μg h/mL of breviscapine, respectively, in comparison to 0.11±0.02 μg h/mL from the commercial breviscapine injection. The ratios of the brain AUC for scutellarin in comparison with the plasma scutellarin AUC for commercial breviscapine injection, Bre-GBSLN-PS, and Bre-GBSLN-PS-DSPE were 0.66%, 2.82%, and 4.51%, respectively. These results showed that though both SLN formulations increased brain uptake of breviscapine, Bre-GBSLN-PS-DSPE which was coated with a binary combination of PEG-40 stearate and DSPE-PEG 2000 had a better brain bioavailability than Bre-GBSLN-PS. Thus, the coating of SLNs with the appropriate PEG derivative combination could improve brain bioavailability of breviscapine and can be a promising tool for brain drug delivery.

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“…The percentage of FBP entrapment in niosomes was analyzed by UV spectrophotometer at 250 nm. The percentage of entrapped FBP was calculated by applying the following equation: where, FBP E is the amount of entrapped drug, and FBP I the initial amount of drug (Lv et al. , 2005; Attia et al.…”

Section: Methodsmentioning

confidence: 99%

The disposition of free and niosomally encapsulated Rac-flurbiprofen in dairy bovines

Confalonieri¹,

Soraci²,

Becaluba³

et al. 2010

Journal of Veterinary Pharmacology and Therapeutics

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Pharmacokinetic parameters were established for flurbiprofen (FBP) after intravenous (i.v.) administration (0.5 mg/kg) of niosomal and nonniosomal formulations in dairy cattle. Niosomes of FBP showed a drug loading of 92.0 +/- 0.7% and the intravenous administration of the FBP niosomes to dairy cattle did not produce any immunological reaction associated to niosomal components. Niosomal FBP was slowly eliminated from plasma and mean residual time (MRT) and AUC(0-->t) and t (1/2) values were significantly higher than those for non niosomal FBP formulations. The results presented in this study indicate that the long circulation of FBP niosomes offers a potential application for improving the pharmacokinetic parameters of short half-life drugs for clinical use. Niosomes offer new promising perspectives of drug delivery modules in bovine therapeutics.

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Distribution of liposomal breviscapine in brain following intravenous injection in rats

Cited by 27 publications

References 2 publications

Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Development of ionic-complex-based nanostructured lipid carriers to improve the pharmacokinetic profiles of breviscapine

Mixed Polyethylene Glycol-Modified Breviscapine-Loaded Solid Lipid Nanoparticles for Improved Brain Bioavailability: Preparation, Characterization, and In Vivo Cerebral Microdialysis Evaluation in Adult Sprague Dawley Rats

The disposition of free and niosomally encapsulated Rac-flurbiprofen in dairy bovines

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