scholarly journals Pharmacokinetic and Tissue Distribution Study of Solid Lipid Nanoparticles of Zidovudine in Rats

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Shah Purvin ◽  
Parameswara Rao Vuddanda ◽  
Sanjay Kumar Singh ◽  
Achint Jain ◽  
Sanjay Singh
Keyword(s):  
Oral Administration ◽  
Tissue Distribution ◽  
Solid Lipid Nanoparticles ◽  
High Performance ◽  
Lipid Nanoparticles ◽  
Peroral Administration ◽  
Pharmacokinetic Parameters ◽  
Distribution Study ◽  
Solid Lipid ◽  
Tissue Distribution Study

Zidovudine-loaded solid lipid nanoparticles (AZT-SLNs) and zidovudine in solution were prepared and administered in rats. The aim of this research was to study whether the bioavailability of zidovudine can be improved by AZT-SLNs perorally to rats as compared to oral administration of zidovudine. Zidovudine was determined in plasma and tissues by reverse phase high performance liquid chromatography. The pharmacokinetic parameters of zidovudine were determined after peroral administration: area under curve of concentration versus time (AUC) for AZT-SLNs was 31.25% greater than AZT solution; meanwhile mean resident time (MRT) was found to be 1.83 times higher for AZT-SLNs than AZT solution. Elimination half life of zidovudine was also increased for SLN formulation. Tissue distribution pattern of zidovudine was changed in case of AZT-SLNs. AUC of zidovudine in brain and liver was found to be approximately 2.73 and 1.77 times higher in AZT-SLNs than AZT solution, respectively, indicating that AZT-SLNs could cross blood brain barrier. Distribution of zidovudine was approximately 0.95 and 0.86 times lesser in heart and kidney, respectively. It can be concluded from the study that oral administration of AZT-SLNs modifies the plasma pharmacokinetic parameters and biodistribution of zidovudine.

scholarly journals Pharmacokinetics and Tissue Distribution Study of Pinosylvin in Rats by Ultra-High-Performance Liquid Chromatography Coupled with Linear Trap Quadrupole Orbitrap Mass Spectrometry

2018 ◽  
Vol 2018 ◽  
pp. 1-14 ◽  
Author(s):  
Yuhang Fu ◽  
Xiaoya Sun ◽  
Lili Wang ◽  
Suiqing Chen
Keyword(s):  
Mass Spectrometry ◽  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
Tissue Distribution ◽  
High Performance ◽  
Gastric Ulcers ◽  
Pharmacokinetic Parameters ◽  
Distribution Study ◽  
Tissue Distribution Study

Pinosylvin is a potential anti-inflammatory and antioxidant compound and the major effective medicinal ingredient in the root of Lindera reflexa Hemsl. However, few investigations have been conducted regarding the pharmacokinetics, excretion, characteristics of tissue distribution, and major metabolites of pinosylvin in rats after oral administration. To better understand the behavior and mechanisms of action underlying the activity of pinosylvin in vivo, we established a simple, sensitive, and reliable ultra-high-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method for quantifying pinosylvin in rat plasma, urine, feces, and various tissues (including heart, liver, spleen, lung, kidneys, large intestine, small intestine, and stomach). Noncompartmental pharmacokinetic parameters indicated that pinosylvin is rapidly distributed and taken up by tissues. The time to peak (maximum) concentration (Tmax) was 0.137 h, and the apparent elimination half-life (t1/2) was 1.347±0.01 h. The results of the tissue distribution study suggest that pinosylvin is widely distributed to various tissues; the highest concentration was observed after 10 min in the stomach, followed by the heart, lung, spleen, and kidneys. Results of the excretion study suggest that a small amount of pinosylvin is excreted from the urine and feces in the parent form; the 73 h accumulative excretion ratios of urine and feces were 0.82% and 0.11%, respectively. It is likely that pinosylvin is mostly metabolized in vivo. Nine metabolites were found, and the main metabolic pathways of pinosylvin in rats included glucuronidation, hydroxylation, and methylation. Four metabolites had higher concentrations in the stomach, suggesting that the stomach is a potential target organ of pinosylvin. In conclusion, the present study may provide a material basis for studying the pharmacological action of pinosylvin and provides meaningful information for the clinical treatment of chronic gastritis and gastric ulcers using Radix Linderae Reflexae.

Pharmacokinetics and Tissue Distribution Study of Ferruginol in Wistar Rat by High-performance Liquid Chromatography

2018 ◽  
Vol 15 (1) ◽  
pp. 67-73 ◽  
Author(s):  
Guiyun Cao ◽  
Suqiao Han ◽  
Keke Li ◽  
Li Shen ◽  
Xiaohong Wang ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
Mobile Phase ◽  
High Performance ◽  
Wistar Rat ◽  
Freezing And Thawing ◽  
Promising Candidate ◽  
Distribution Study ◽  
Substance Loss ◽  
Tissue Distribution Study ◽  
The Brain

Background: Ferruginol (FRGN) exhibits a broad range of pharmacological properties which make it a promising candidate for chemoprevention. However, little is known about its absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties. Methods: A rapid, sensitive and specific HPLC-DAD method was established to quantify FRGN in the plasma and tissues of Wistar rats. After extraction of FRGN with ethyl acetate (EtOAc), chromatographic separation was performed on a YMC ODS C18 column (250 × 4.6 mm I.D., 5 µm) with a mobile phase consisting of methanol-water (92:8, v/v) at a flow rate of 0.9 mL/min. Detection was conducted with a wavelength of 273 nm at 25 °C. Results: The calibration curves for FRGN were linear in the concentration range of 0.5-20 µg/mL for plasma, 0.5-10 µg/mL for heart, liver, spleen, lung, kidney, stomach, intestine, brain and muscle. After three cycles of freezing and thawing, the concentration variations were within ± 7% of nominal concentrations, indicating no significant substance loss during repeated thawing and freezing. The assay was applied to pharmacokinetic and tissue distribution study in rats. Results suggested that lung, heart, liver, spleen and kidney were the major distribution tissues of FRGN in rats, and FRGN could permeate the blood-brain barrier to distribute in the brain of rats. Conclusion: The information provided by this research is very useful for gaining knowledge of the pharmacokinetic process and tissue distribution of FRGN.

scholarly journals Targeting the Endocannabinoid/CB1 Receptor System For Treating Major Depression Through Antidepressant Activities of Curcumin and Dexanabinol-Loaded Solid Lipid Nanoparticles

2017 ◽  
Vol 42 (6) ◽  
pp. 2281-2294 ◽  
Author(s):  
Xiaolie He ◽  
Li Yang ◽  
Mei Wang ◽  
Xizhen Zhuang ◽  
Ruiqi Huang ◽  
...  
Keyword(s):  
Major Depression ◽  
Solid Lipid Nanoparticles ◽  
High Performance ◽  
Apoptotic Cell ◽  
Lipid Nanoparticles ◽  
Mrna Levels ◽  
Neuroprotective Effects ◽  
Receptor System ◽  
Solid Lipid

Background/Aims: This study investigated the underlying mechanisms of the antidepressant effects of curcumin and dexanabinol-loaded solid lipid nanoparticles in corticosterone-induced cell and mice depression models. Methods: Curcumin and dexanabinol-loaded solid lipid nanoparticles (Cur/SLNs-HU-211) were synthesized via an emulsifcation and low-temperature solidification method. Antidepressant activities of nanoparticles in a corticosterone-induced major depression model were investigated by MTT assay, cellular uptake by flow cytometry, behaviour by Forced Swimming Test and rotarod test, neurotransmitters by High Performance Liquid Chromatography, Western blotting, qPCR and immunofluorescence. Results: Treatment with Cur/SLNs-HU-211 induced greater dopamine (DA)/5-hydroxytryptamine (5-HT) release with reduced corticosterone-induced apoptotic cell death in PC12 cells. Additionally, in vivo Cur/SLNs-HU-211 significantly induced recovery from depressive behaviour with increased DA/5-HT levels, CB1 mRNA levels and CB1, p-MEK1 and p-ERK1/2 protein expression levels in the hippocampus and striatum. Cur/SLNs-HU-211 improved CB1 expression and inspired the proliferation of astrocytes in the hippocampus and striatum, exerted neuroprotective effects by preventing corticosterone -induced BDNF/NeuN expression reduction. Conclusion: Our study implies that Cur/SLNs-HU-211 may be a useful approach for treatment of major depression.

scholarly journals Simultaneous Measurement of Tadehaginoside and its Principal Metabolite in Rats by HPLC–MS/MS and its Application in Pharmacokinetics and Tissue Distribution Study

2021 ◽  
Author(s):  
Cai-Yun Zhang ◽  
Ya-Ting Lu ◽  
Yin-Feng Tan ◽  
Lin Dong ◽  
Zhi-Heng Su ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
High Performance ◽  
Biological Activities ◽  
Intragastric Administration ◽  
Distribution Study ◽  
Chromatography Tandem Mass Spectrometry ◽  
Liquid Chromatography Tandem Mass ◽  
Tissue Distribution Study

Abstract Background Tadehaginoside, an active ingredient isolated from Tadehagi triquetrum L., exhibited various biological activities. However, the pharmacokinetics and tissue-distribution which affects tadehaginoside’s therapeutic actions and application remain elusive.MethodsTo clarify the metabolism of tadehaginoside in vivo, a high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was established to detect the level of tadehaginoside in plasma and eleven tat tissues (brain, heart, liver, spleen, lungs, kidneys, stomach, small intestine, skeletal muscle, body fat, and testes). Besides, this validated method was also successfully applied to the quantitative determination of its metabolite, p-hydroxycinnamic acid (HYD) in plasma. The pharmacokinetic and tissue-distribution of tadehaginoside were investigated by this developed method. ResultsThe pharmacokinetic study indicated that tadehaginoside in plasma of rats with intragastric administration showed relatively low concentration may be due to the formation of its metabolite, and the quick absorption of tadehaginoside was detected following intravenous administration. Tissue-distribution study indicated that kidney and spleen were the major distribution organs for tadehaginoside in rats. ConclusionsThese results could provide clues for exploring the bioactivity of tadehaginoside based on its pharmacokinetic characteristics.

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