Abstract

Itraconazole, a broad-spectrum anti-fungal, has many side effects, and nanosystems for drug delivery have been proposed as a method to optimize the drug's pharmacokinetics and reduce side effects. An high performance liquid chromatography (HPLC) procedure using fluorometric detection was developed for determination of itraconazole in polymeric poly(lactic-co-glycolic acid) nanoparticles, plasma and tissue. Linearity, limits of detection and quantification, recovery, precision, selectivity and stability were established. The developed method was tested in itraconazole detection and quantification of biodistribution of nanoparticles administered intraperitoneally to Balb/C female mice. This study developed an analytical method for HPLC with fluorometric detection for quantification of itraconazole in polymeric nanoparticles, tissue and plasma, which is sensitive, low cost, viable for routine usage and with potential for application in itraconazole biodistribution and pharmacokinetics studies.

Highlights

  • Itraconazole (ITZ) (Figure 1) is a classical member of the triazole class that exhibits a broad-spectrum antifungal activity.[1]

  • Optimum mobile phase composition was determined by analysis of ITZ and internal standard (IS) peaks in water/solvent gradients in a standard C-18 column

  • The retention time of ITZ and IS was decisive for definition of isocratic mobile phase used throughout experiments: acetonitrile: water (50:50, with 0.12% Trifluoracetic acid (TFA))

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Summary

Introduction

Itraconazole (ITZ) (Figure 1) is a classical member of the triazole class that exhibits a broad-spectrum antifungal activity.[1].

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