Titre du document / Document title

Intravitreal pharmacokinetics of plain and liposome-entrapped fluconazole in rabbit eyes

Auteur(s) / Author(s)

GUPTA S. K. ⁽¹⁾ ; VELPANDIAN T. ⁽¹⁾ ; DHINGRA N. ⁽¹⁾ ; JAISWAL J. ⁽¹⁾ ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

⁽¹⁾ Department of Pharmacology, All India Institute of Medical Sciences (AIIMS), New Delhi, INDE

Résumé / Abstract

The objective of our experiment was to study the pharmacokinetics of plain and liposome-encapsulated fluconazole after an intravitreal injection (100 μg/0.1 ml) in rabbit eyes. Equal concentrations of plain and liposome-entrapped fluconazole were injected intravitreally into albino rabbits through the pars plana after intravenous pentobarbitone anesthesia. The rabbits were sacrificed at various time intervals, and the concentration of fluconazole in vitreous, retinachoroid, aqueous humor and cornea was estimated using High Performance Liquid Chromatography (HPLC). Plain fluconazole showed a rapid vitreal clearance and a short half-life (3.08 hr), whereas liposome-entrapped fluconazole showed a longer half-life (23. 40 hr). The terminal elimination constant (Ke) ofthe liposome-loaded drug from the vitreous was seven times less than the plain drug. In the plain fluconazole group, at 1 hr, a high concentration of the drug was found in the retina. To conclude, the elimination of fluconazole was primarily transretinal and was very rapid. Liposome encapsulation significantly increased the half-life of fluconazole in the vitreous cavity.

Revue / Journal Title

Journal of ocular pharmacology and therapeutics   ISSN 1080-7683 

Source / Source

2000, vol. 16, n^o6, pp. 511-518 (14 ref.)

Langue / Language

Anglais

Editeur / Publisher

Liebert, Larchmont, NY, ETATS-UNIS  (1995) (Revue)

Mots-clés anglais / English Keywords

Fluconazole ; Antifungal agent ; Intravitreous administration ; Pharmacokinetics ; Rabbit ; Animal ; Dosage form ; Encapsulation ; Liposome ; Controlled release form ; Triazole derivatives ; Lagomorpha ; Mammalia ; Vertebrata ;

Mots-clés français / French Keywords

Fluconazole ; Antifongique ; Voie intravitréenne ; Pharmacocinétique ; Lapin ; Animal ; Forme pharmaceutique ; Encapsulation ; Liposome ; Forme libération contrôlée ; Triazole dérivé ; Lagomorpha ; Mammalia ; Vertebrata ;

Mots-clés espagnols / Spanish Keywords

Fluconazol ; Antifúngico ; Vía intravítrea ; Farmacocinética ; Conejo ; Animal ; Forma farmacéutica ; Encapsulación ; Liposoma ; Forma liberación controlada ; Triazol derivado ; Lagomorpha ; Mammalia ; Vertebrata ;

Localisation / Location

INIST-CNRS, Cote INIST : 20947, 35400009354052.0020