A stepwise optimization strategy to formulate in situ gelling formulations comprising fluconazole-hydroxypropyl-beta-cyclodextrin complex loaded niosomal vesicles and Eudragit nanoparticles for enhanced antifungal activity and prolonged ocular delivery

Asian Journal of Pharmaceutical Sciences
Heba Elmotasem, Ghada E A Awad

Abstract

Fungal keratitis and endopthalmitis are serious eye diseases. Fluconazole (FL) is indicated for their treatment, but suffers from poor topical ocular availability. This study was intended to improve and prolong its ocular availability. FL niosomal vesicles were prepared using span 60. Also, polymeric nanoparticles were prepared using cationic Eudragit RS100 and Eudragit RL100. The investigated particles had adequate entrapment efficiency (EE%), nanoscale particle size and high zeta potential. Subsequently, formulations were optimized using full factorial design. FL-HP-β-CD complex was encapsulated in selected Eudragit nanoprticles (FL-CD-ERS1) and niosmal vesicles. The niosomes were further coated with cationic and bioadhesive chitosan (FL-CD-Nios-ch). EE% for FL-CD-ERS1 and FL-CD-Nios-ch formulations were 76.4% and 61.7%; particle sizes were 151.1 and 392 nm; also, they exhibited satisfactory zeta potential +40.1 and +28.5 mV. In situ gels were prepared by poloxamer P407, HPMC and chitosan and evaluated for gelling capacity, rheological behavior and gelling temperature. To increase the precorneal residence time, free drug and selected nano-formulations were incorporated in the selected in situ gel. Release study revealed susta...Continue Reading

Citations

Oct 21, 2020·Journal of Drug Delivery Science and Technology·Juliana Rincón-LópezYareli Rojas-Aguirre
Apr 12, 2021·Drug Delivery and Translational Research·Wenjie FanKe Yao
May 27, 2021·Human & Experimental Toxicology·M S SamimiM Mohammadi
Jun 29, 2021·Pharmaceutical Development and Technology·Tarek Metwally IbrahimHanan Mohammed El-Nahas
Jul 12, 2021·International Journal of Pharmaceutics·Beatriz SilvaLídia Gonçalves

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Methods Mentioned

BETA
nanoprecipitation
dynamic light scattering
transmission electron microscopy
X-ray
transmission
scanning electron microscopy

Software Mentioned

Design
SPSS
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