Novel bioanalytical method for the quantification of rufinamide in mouse plasma and tissues using HPLC-UV: A tool to support pharmacokinetic studies

Meirinho, Sara; Rodrigues, Márcio; Fortuna, Ana; Falcão, Amílcar; Alves, Gilberto

doi:10.1016/j.jchromb.2019.06.021

Cited by 9 publications

(6 citation statements)

References 34 publications

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“…Each group of 39 mice was administered with a single dose of 10.0 mg/kg of free OXA, L-OXA, or ES-SSL-OXA via tail vein injection, respectively. At different time points (n=3) 50 , 51 of 5, 10, 15, and 30 min, 1, 2, 4, 6, 8, 12, 24, 36, and 48 h after IV injection, 0.5 mL of blood sample of each mouse was collected into heparinized tubes. The animals were sacrificed and dissected to collect main organs of heart, liver, spleen, lungs, and kidneys.…”

Section: Methodsmentioning

confidence: 99%

In vitro and in vivo Evaluation of a Novel Estrogen-Targeted PEGylated Oxaliplatin Liposome for Gastric Cancer

Sun¹,

Xie²,

Tang³

et al. 2021

IJN

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Background: Chemotherapy is still the main first-line treatment for advanced metastatic gastric cancer, but it has the limitations of serious side effects and drug resistance. Conventional liposome has been substantially used as drug carriers, but they lack targeting character with lower drug bioavailability in tumor tissues. Based on the above problems, a novel estrogentargeted PEGylated liposome loaded with oxaliplatin (ES-SSL-OXA) was prepared to further improve the metabolic behavior, the safety profile, and the anti-tumor efficacy of oxaliplatin. Methods: Four kinds of oxaliplatin (OXA) liposomes were prepared by film hydration method. The obtained formulations were characterized in terms of entrapment efficiency (EE), particle size, and so on by HPLC and DLS (dynamic light scanning). The morphology of ES-SSL-OXA was detected by transmission electron microscope (TEM). The in vitro and in vivo targeting effect of ES-SSL-OXA was verified by fluorescence microscopy and in vivo imaging system in gastric cancer cells (SGC-7901) and tumor-bearing athymic mice. The in vitro and in vivo antitumor efficacies of ES-SSL-OXA were investigated on SGC-7901 cells and athymic tumor-bearing mice. Pharmacokinetic, biodistribution, and acute toxicity tests of ES-SSL-OXA were performed on ICR mice. Results:The ES-SSL-OXA exhibited an average particle size of about 153.37 nm with an encapsulation efficiency of 46.20% and low leakage rates at 4°C and 25°C. In vivo and in vitro targeting study confirmed that ES-SSL-OXA could effectively target the tumor site. The antitumor activity demonstrated the strongest inhibition in tumor growth of ES-SSL-OXA. Pharmacokinetics and acute toxicity study showed that ES-SSL-OXA could significantly improve the metabolic behavior and toxicity profile of oxaliplatin. Conclusion:In this study, a novel estrogen-targeted long-acting liposomal formulation of OXA was successfully prepared. ES fragment effectively targeted the delivery system to tumor tissues which highly express estrogen receptor, providing a promising therapeutic method for gastric cancer in clinic.

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Section: Methodsmentioning

confidence: 99%

In vitro and in vivo Evaluation of a Novel Estrogen-Targeted PEGylated Oxaliplatin Liposome for Gastric Cancer

Sun¹,

Xie²,

Tang³

et al. 2021

IJN

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“…After type C discharges, there is usually a period of marked postictal suppression, both electrophysiologically and behaviorally, for several seconds to minutes. Rufinamide (50mg/kg, roughly corresponding to serum levels in therapeutic conditions 40,41 ) markedly decreases type B and C, but not type A discharges. Type A discharges are even increased, presumably ascribable to the "truncated" type B and type C discharges and suggestive of the ultimate ineffectiveness of rufinamide on the ultrashort bursts or depolarization.…”

Section: Rufinamide Is Distinctively Effective Against Swds In Vivomentioning

confidence: 97%

“…This is consistent with the clinical experiences of ineffectiveness or even aggravation of myoclonic jerks in LGS with rufinamice. 41 In contrast, phenytoin (40mg/kg, resulting in serum levels roughly corresponding to those in therapeutic conditions 34,35 ) shows no effect on type B and type C discharges. Behaviorally, the seizures associated with type B and type C are consistently decreased by rufinamide but not phenytoin.…”

Section: Rufinamide Is Distinctively Effective Against Swds In Vivomentioning

confidence: 98%

How Can an Na⁺ Channel Inhibitor Ameliorate Seizures in Lennox–Gastaut Syndrome?

Lin

Lai

Chou

et al. 2021

Annals of Neurology

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Objective Lennox–Gastaut syndrome (LGS) is an epileptic encephalopathy frequently associated with multiple types of seizures. The classical Na+ channel inhibitors are in general ineffective against the seizures in LGS. Rufinamide is a new Na+ channel inhibitor, but approved for the treatment of LGS. This is not consistent with a choice of antiseizure drugs (ASDs) according to simplistic categorical grouping. Methods The effect of rufinamide on the Na+ channel, cellular discharges, and seizure behaviors was quantitatively characterized in native neurons and mammalian models of epilepsy, and compared with the other Na+ channel inhibitors. Results With a much faster binding rate to the inactivated Na+ channel than phenytoin, rufinamide is distinctively effective if the seizure discharges chiefly involve short bursts interspersed with hyperpolarized interburst intervals, exemplified by spike and wave discharges (SWDs) on electroencephalograms. Consistently, rufinamide, but not phenytoin, suppresses SWD‐associated seizures in pentylenetetrazol or AY‐9944 models, which recapitulate the major electrophysiological and behavioral manifestations in typical and atypical absence seizures, including LGS. Interpretation Na+ channel inhibitors shall have sufficiently fast binding to exert an action during the short bursts and then suppress SWDs, in which cases rufinamide is superior. For the epileptiform discharges where the interburst intervals are not so hyperpolarized, phenytoin could be better because of the higher affinity. Na+ channel inhibitors with different binding kinetics and affinity to the inactivated channels may have different antiseizure scope. A rational choice of ASDs according to in‐depth molecular pharmacology and the attributes of ictal discharges is advisable. ANN NEUROL 2021;89:1099–1113

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“…RFM monitoring level is beneficial because of a good correlation between serum drug level and seizure control to individual needs [4,5,125,187,188]. RFM level is detected by LC coupled with UV or MS detection [189][190][191]. Linear ranges are 0.005-50 mg/L.…”

Section: Rufinamidementioning

confidence: 99%

New Methods Used in Pharmacokinetics and Therapeutic Monitoring of the First and Newer Generations of Antiepileptic Drugs (AEDs)

et al. 2020

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The review presents data from the last few years on bioanalytical methods used in therapeutic drug monitoring (TDM) of the 1st–3rd generation and the newest antiepileptic drug (AEDs) cenobamate in patients with various forms of seizures. Chemical classification, structure, mechanism of action, pharmacokinetic data and therapeutic ranges for total and free fractions and interactions were collected. The primary data on bioanalytical methods for AEDs determination included biological matrices, sample preparation, dried blood spot (DBS) analysis, column resolution, detection method, validation parameters, and clinical utility. In conclusion, the most frequently described method used in AED analysis is the LC-based technique (HPLC, UHPLC, USLC) combined with highly sensitive mass detection or fluorescence detection. However, less sensitive UV is also used. Capillary electrophoresis and gas chromatography have been rarely applied. Besides the precipitation of proteins or LLE, an automatic SPE is often a sample preparation method. Derivatization was also indicated to improve sensitivity and automate the analysis. The usefulness of the methods for TDM was also highlighted.

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Novel bioanalytical method for the quantification of rufinamide in mouse plasma and tissues using HPLC-UV: A tool to support pharmacokinetic studies

Cited by 9 publications

References 34 publications

In vitro and in vivo Evaluation of a Novel Estrogen-Targeted PEGylated Oxaliplatin Liposome for Gastric Cancer

In vitro and in vivo Evaluation of a Novel Estrogen-Targeted PEGylated Oxaliplatin Liposome for Gastric Cancer

How Can an Na⁺ Channel Inhibitor Ameliorate Seizures in Lennox–Gastaut Syndrome?

New Methods Used in Pharmacokinetics and Therapeutic Monitoring of the First and Newer Generations of Antiepileptic Drugs (AEDs)

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Novel bioanalytical method for the quantification of rufinamide in mouse plasma and tissues using HPLC-UV: A tool to support pharmacokinetic studies

Cited by 9 publications

References 34 publications

In vitro and in vivo Evaluation of a Novel Estrogen-Targeted PEGylated Oxaliplatin Liposome for Gastric Cancer

In vitro and in vivo Evaluation of a Novel Estrogen-Targeted PEGylated Oxaliplatin Liposome for Gastric Cancer

How Can an Na+ Channel Inhibitor Ameliorate Seizures in Lennox–Gastaut Syndrome?

New Methods Used in Pharmacokinetics and Therapeutic Monitoring of the First and Newer Generations of Antiepileptic Drugs (AEDs)

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How Can an Na⁺ Channel Inhibitor Ameliorate Seizures in Lennox–Gastaut Syndrome?