Validated liquid chromatographic determination of 5-fluorouracil in human plasma

Alsarra, Ibrahim A.; Al-Arifi, Mohammed N.

doi:10.1016/j.jchromb.2004.01.043

Cited by 43 publications

(13 citation statements)

References 15 publications

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“…For infusion studies, mice received an infusion of 5-FU (13 mg/kg/hour) via subcutaneous Alzet pumps (model 2001D; Cupertino, CA) and blood samples were taken at 24, 48, and 72 hours post pump implantation. 5-FU levels were determined in blood samples using a modified previously described HPLC method (Alsarra and Alarifi, 2004). Penetration of 5-FU into orthotopically implanted mEP Ephb2 brain tumors following intravenous bolus or subcutaneous infusion was assessed using a previously published microdialysis technique (Zhuang et al, 2006).…”

Section: Methodsmentioning

confidence: 99%

An Integrated In Vitro and In Vivo High-Throughput Screen Identifies Treatment Leads for Ependymoma

et al. 2011

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Summary Using a mouse model of ependymoma—a chemoresistant brain tumor—we combined multi-cell high-throughput screening (HTS), kinome-wide binding assays, and in vivo efficacy studies, to identify potential treatments with predicted toxicity against neural stem cells (NSC). We identified kinases within the insulin signaling pathway and centrosome cycle as regulators of ependymoma cell proliferation, and their corresponding inhibitors as potential therapies. FDA approved drugs not currently used to treat ependymoma were also identified that posses selective toxicity against ependymoma cells relative to normal NSCs both in vitro and in vivo e.g., 5-fluoruracil. Our comprehensive approach advances understanding of the biology and treatment of ependymoma including the discovery of several treatment leads for immediate clinical translation.

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Section: Methodsmentioning

confidence: 99%

An Integrated In Vitro and In Vivo High-Throughput Screen Identifies Treatment Leads for Ependymoma

et al. 2011

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“…The HPLC system (LC-10AT VP, Shimadzu liquid chromatograph, Shimadzu, Kyoto, Japan) consisted of SPDM10AVP Shimadzu diode array detector, and a Luna 5m C18 column (250 mm Â 4.60 mm) was used for the analysis of drug. The mobile phase was water:methanol (95:5 v/v) pumped at a flow rate of 1 mL/min at 25 C. The mobile phase was out-gassed under vacuum before use (Alsarra & Alarifi, 2004). The detection wavelength was 266 nm.…”

Section: Drug Entrapment Efficiencymentioning

confidence: 99%

Eudragit-coated dextran microspheres of 5-fluorouracil for site-specific delivery to colon

et al. 2014

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Objective of the present investigation was to prepare and evaluate the potential of enteric coated dextran microspheres for colon targeting of 5-fluorouracil (5-FU). Dextran microspheres were prepared by emulsification-crosslinking method and the formulation variables studied included different molecular weights of dextran, drug:polymer ratio, volume of crosslinking agent, stirring speed and time. Enteric coating (Eudragit S-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method using different coat:core ratios (4:1 or 8:1). Uncoated and coated dextran microspheres were characterized by particle size, surface morphology, entrapment efficiency, DSC, in vitro drug release in the presence of dextranase and 2% rat cecal contents. The release study of 5-FU from coated dextran microspheres was pH dependent. No release was observed at acidic pH; however, the drug was released quickly where Eudragit starts solublizing there was continuous release of drug from the microspheres. Organ distribution study was suggested that coated dextran microspheres retard the release of drug in gastric and intestinal pH environment and released of drug from microspheres in colon due to the degradation of dextran by colonic enzymes.

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“…Following, the epidermis or dermis sample pieces were mixed with 1 mL of physiological saline and subjected to homogenization for 3 min. The amount of 5-FU in the blood, epidermis or dermis samples was analyzed by HPLC method (Agilent Technologies) (Alsarra & Alarifi, 2004), respectively.…”

Section: Blood Level Studymentioning

confidence: 99%

In-vitroandin-vivoassessment of dextran-appended cellulose acetate phthalate nanoparticles for transdermal delivery of 5-fluorouracil

Garg¹,

Rai²,

Lodhi³

et al. 2014

Drug Delivery

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The aim of this research was transdermal delivery of 5-fluorouracil (5-FU) using dextran-coated cellulose acetate phthalate (CAP) nanoparticulate formulation. CAP nanoparticles were prepared using drug-polymer ratio (1:1 to 1:3) and surfactant ratio (2.5, 5 and 10%). Dextran coating was made using aminodextran. The results showed that the optimized CAP nanoparticles (CNs) and dextran-coated CAP nanoparticles represented core-corona nanoparticles with the mean diameter of 75 ± 3 and 79 ± 2 nm, respectively, and entrapment efficiency was 82.5 ± 0.06 and 78.2 ± 0.12, respectively. Dextran-coated nanoparticles (FDCNs) and CAP nanoparticles (FCNs) showed in vitro 5-FU release upto 31 h and 8 h, respectively. Moreover, the cumulative amount of 5-FU penetrated through excised skin from FDCNs was 2.94 folds than that of the FU cream. Concentration of 5-FU in epidermis and dermis were also studied. In dermis, concentration of 5-FU was found higher in case of FDCN formulation than plain FU cream. FDCNs were found more hemocompatible in comparison to FCNs. The hematological data recommended that FDCNs formulation was less immunogenic compared to FU creams formulation. In blood level study, FDCNs exhibited 153, 12, 16.66 and 16.24-fold higher values for area under the curve, Tmax, Cmax and mean residence time (MRT) compared with those of FU cream, respectively. The in-vitro cytotoxicity was assessed using the MCF-7 by the MTT test and was compared to the plain 5-FU solution. All the detailed evidence showed that FDCNs could provide a promising tuning as a transdermal delivery system of 5-FU.

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Validated liquid chromatographic determination of 5-fluorouracil in human plasma

Cited by 43 publications

References 15 publications

An Integrated In Vitro and In Vivo High-Throughput Screen Identifies Treatment Leads for Ependymoma

An Integrated In Vitro and In Vivo High-Throughput Screen Identifies Treatment Leads for Ependymoma

Eudragit-coated dextran microspheres of 5-fluorouracil for site-specific delivery to colon

In-vitroandin-vivoassessment of dextran-appended cellulose acetate phthalate nanoparticles for transdermal delivery of 5-fluorouracil

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