Validated High-Performance Liquid Chromatographic Technique for Determination of 5-Fluorouracil: Applications to Stability Studies and Simulated Colonic Media

Alanazi, Fars K.; Yassin, Alaa Eldeen B.; El-Badry, Mahmoud; Mowafy, Hammam A.; Alsarra, Ibrahim A.

doi:10.1093/chromsci/47.7.558

Cited by 27 publications

(20 citation statements)

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“…It showed a high linearity of the standard calibration curve of 5-FU in the rat caecal content with a R 2 value of 0.998 in the concentration range from 0.5 to 5 µg/ml 31.…”

Section: Resultsmentioning

confidence: 87%

“…The slow release profile exhibited by the drug may be ascribed by the lower solubility of 5-FU (0.1M ) in neutral phosphate buffers 41. The high stability of 5-FU in rat caecal content medium was reported in a previous study 31. Paharia et al 42 studied the release of 5-FU from Eudragit-coated pectin microspheres in a simulated colonic medium containing rat caecal contents under anaerobic conditions.…”

Section: Resultsmentioning

confidence: 89%

“…A simple and sensitive stability-indicating HPLC method with a UV detection using thymine as an internal standard was adopted 31. The method was utilized for the assessment of stability of 5-FU in rat caecal content as simulated colon medium under anaerobic conditions.…”

Section: Methodsmentioning

confidence: 99%

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Optimization of 5-fluorouracil solid-lipid nanoparticles: a preliminary study to treat colon cancer

Yassin¹,

Anwer²,

Mowafy³

et al. 2010

Int. J. Med. Sci.

167

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Solid lipid nanoparticle (SLNs) formulae were utilized for the release of 5-flurouracil (5-FU) inside the colonic medium for local treatment of colon cancer. SLNs were prepared by double emulsion-solvent evaporation technique (w/o/w) using triglyceride esters, Dynasan™ 114 or Dynasan™ 118 along with soyalecithin as the lipid parts. Different formulation parameters; including type of Dynasan, soyalicithin:Dynasan ratio, drug:total lipid ratio, and polyvinyl alcohol (PVA) concentration were studied with respect to particle size and drug entrapment efficiency. Results showed that formula 8 (F8) with composition of 20% 5-FU, 27% Dynasan™ 114, and 53% soyalithicin and F14 (20% 5-FU, 27% Dynasan™ 118, and 53% soyalithicin), which were stabilized by 0.5% PVA, as well as F10 with similar composition as F8 but stabilized by 2% PVA were considered the optimum formulae as they combined small particle sizes and relatively high encapsulation efficiencies. F8 had a particle size of 402.5 nm ± 34.5 with a polydispersity value of 0.005 and an encapsulation efficiency of 51%, F10 had a 617.3 nm ± 54.3 particle size with 0.005 polydispersity value and 49.1% encapsulation efficiency, whereas formula F14 showed a particle size of 343 nm ± 29 with 0.005 polydispersity, and an encapsulation efficiency of 59.09%. DSC and FTIR results suggested the existence of the lipids in the solid crystalline state. Incomplete biphasic prolonged release profile of the drug from The three formulae was observed in phosphate buffer pH 6.8 as well as simulated colonic medium containing rat caecal contents. A burst release with magnitudes of 26%, 32% and 28.8% cumulative drug released were noticed in the first hour samples incubated in phosphate buffer pH 6.8 for both F8, F10 and F14, respectively, followed by a slow release profile reaching 50%, 46.3% and 52% after 48 hours.

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“…It showed a high linearity of the standard calibration curve of 5-FU in the rat caecal content with a R 2 value of 0.998 in the concentration range from 0.5 to 5 µg/ml 31.…”

Section: Resultsmentioning

confidence: 87%

Section: Resultsmentioning

confidence: 89%

See 1 more Smart Citation

Optimization of 5-fluorouracil solid-lipid nanoparticles: a preliminary study to treat colon cancer

Yassin¹,

Anwer²,

Mowafy³

et al. 2010

Int. J. Med. Sci.

167

View full text Add to dashboard Cite

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“…The bag was suspended in a beaker containing 100 ml of a saline phosphate buffer (pH 7.4) under continuous stirring using a hot plate magnetic stirrer, maintained at 37±1°C. Samples were withdrawn periodically and replaced with the equivalent volume of the fresh saline phosphate buffer (pH 7.4) and the amount of drug was quantified using an HPLC method [ 39 ].…”

Section: Methodsmentioning

confidence: 99%

Low Density Lipid Nanoparticles for Solid Tumor Targeting

et al. 2014

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One of the most significant characteristics of cancer cells is their rapid dividing ability and overexpression of LDL receptors, which offers an opportunity for the selective targeting of these cells. 5-Fluorouracil (5-FU)-encapsulated low density lipid nanoparticles (LDLN) were prepared by the emulsion congealing method which mimics the plasma-derived LDL by acquiring the apolipoprotein B-100 from the blood. The average particle size, transmission electron microscope (TEM), and drug content of the prepared LDLN dispersion were found to be 161±3.5 nm, with spherical shape, and 0.370±0.05 mg/mL, respectively. In vitro release studies revealed a sustained profile which decreased with a lapse of time. In vivo studies of 5-FU serum concentration and biodistribution revealed a 5-FU serum concentration of 8.5% in tumor cells and about 2.1% in the liver at the end of 24 hr from LDLN. Tumor growth suppression studies showed 185.42% average tumor growth and 89.76% tumor height as compared to the control exhibiting tumor growth at 1166.47% and tumor height at 176.07%. On the basis of these collective data, it is suggested that a higher accumulation of LDLN, when given as an IV, in solid tumors is attributed to the active uptake of LDLN via LDL receptors via apolipoprotein B-100.

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“…5-FU have also been quantified in cultured cell model by LC-MS coupled to MS detection technique over a concentration range of 2.5-150 ng mL -1 , without any matrix effect [46]. A reliable, simple, isocratic stability indicating HPLC-UV method have been developed for 5-FU analysis using thymine as an internal standard within the concentration range of 0.1-2.0 lg mL -1 [47]. A chromatographic analysis for capecitabine and its metabolites (5-FU) was performed on a C18 reverse phase column with detection by atmosphere pressure chemical ionization LC-MS/MS.…”

Section: Hybrid Instrumental Techniques For 5-fu Analysis In Biologicmentioning

confidence: 99%

A Critical Review on Clinical Application of Separation Techniques for Selective Recognition of Uracil and 5-Fluorouracil

2015

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The most important objectives that are frequently found in bio-analytical chemistry involve applying tools to relevant medical/biological problems and refining these applications. Developing a reliable sample preparation step, for the medical and biological fields is another primary objective in analytical chemistry, in order to extract and isolate the analytes of interest from complex biological matrices. Since, main inborn errors of metabolism (IEM) diagnosable through uracil analysis and the therapeutic monitoring of toxic 5-fluoruracil (an important anticancerous drug) in dihydropyrimidine dehydrogenase deficient patients, require an ultra-sensitive, reproducible, selective, and accurate analytical techniques for their measurements. Therefore, keeping in view, the diagnostic value of uracil and 5-fluoruracil measurements, this article refines several analytical techniques involved in selective recognition and quantification of uracil and 5-fluoruracil from biological and pharmaceutical samples. The prospective study revealed that implementation of molecularly imprinted polymer as a solid-phase material for sample preparation and preconcentration of uracil and 5-fluoruracil had proven to be effective as it could obviates problems related to tedious separation techniques, owing to protein binding and drastic interferences, from the complex matrices in real samples such as blood plasma, serum samples.

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Validated High-Performance Liquid Chromatographic Technique for Determination of 5-Fluorouracil: Applications to Stability Studies and Simulated Colonic Media

Cited by 27 publications

References 0 publications

Optimization of 5-fluorouracil solid-lipid nanoparticles: a preliminary study to treat colon cancer

Optimization of 5-fluorouracil solid-lipid nanoparticles: a preliminary study to treat colon cancer

Low Density Lipid Nanoparticles for Solid Tumor Targeting

A Critical Review on Clinical Application of Separation Techniques for Selective Recognition of Uracil and 5-Fluorouracil

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