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<p>Gliclazide, a BCS (Biological Classification System) Class II antidiabetic drug, suffers from poor aqueous solubility and variable bioavailability. Nanoparticle-based delivery systems can improve its pharmacokinetic profile and reduce toxicity. Zebrafish, with significant genomic similarity to humans, provide a promising in vivo model for preclinical screening. The study aims to develop and evaluate the safety and efficacy of gliclazide-loaded nanoparticles (GLNPs) using a zebrafish model. The novelty of this work lies in performing an in vivo zebrafish study to evaluate prepared GLNPs.&#xa0;GLNPs were prepared using the solvent evaporation method. Different formulations were developed by varying the ratio of two polymers—Eudragit RLPO and Eudragit RL100. The optimized formulation (F1) was selected based on drug content, particle size, polydispersity index (PDI), and zeta potential. In vitro drug release, surface morphology (SEM), thermal behavior (DSC), crystallinity (XRD), and compatibility (FT-IR) studies were performed. Toxicity and efficacy studies were conducted using zebrafish embryos.&#xa0;The optimized formulation (F1), prepared with Eudragit RLPO, showed a drug content of 96.68%, entrapment efficiency of 87.5%, particle size of 310.7&#xa0;nm, PDI of 0.212, and a zeta potential of + 25.7 mV. It achieved 93.93% cumulative drug release sustained up to 8&#xa0;h. SEM revealed spherical morphology, while DSC and XRD confirmed retention of the crystalline nature of gliclazide. FT-IR analysis showed no significant drug-excipient interaction. Toxicity studies in zebrafish embryos indicated no significant toxic effects. The developed formulation demonstrated superior safety and efficacy compared to the marketed formulation.&#xa0;The study successfully demonstrated that GLNPs offer a promising alternative for enhancing the oral bioavailability of gliclazide with improved safety and sustained therapeutic efficacy in a zebrafish model.</p> Graphical Abstract <p>Formulation, characterization, antidiabetic evaluation, and toxicity study on zebrafish of gliclazide loaded polymeric nanoparticles</p> <p></p>

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Gliclazide-Loaded Nanoparticles: Antidiabetic Efficacy and Safety in Zebrafish

  • 期刊论文

  • 发表日期：

    2025年12月17日

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  • Swarupananda Mukherjee,
  • Susmita Paul,
  • Suchana Das,
  • Rukaiah Fatma Begum,
  • Sayan Ghosh,
  • Dipanjan Karati,
  • Bhupendra G. Prajapati

摘要

Gliclazide, a BCS (Biological Classification System) Class II antidiabetic drug, suffers from poor aqueous solubility and variable bioavailability. Nanoparticle-based delivery systems can improve its pharmacokinetic profile and reduce toxicity. Zebrafish, with significant genomic similarity to humans, provide a promising in vivo model for preclinical screening. The study aims to develop and evaluate the safety and efficacy of gliclazide-loaded nanoparticles (GLNPs) using a zebrafish model. The novelty of this work lies in performing an in vivo zebrafish study to evaluate prepared GLNPs. GLNPs were prepared using the solvent evaporation method. Different formulations were developed by varying the ratio of two polymers—Eudragit RLPO and Eudragit RL100. The optimized formulation (F1) was selected based on drug content, particle size, polydispersity index (PDI), and zeta potential. In vitro drug release, surface morphology (SEM), thermal behavior (DSC), crystallinity (XRD), and compatibility (FT-IR) studies were performed. Toxicity and efficacy studies were conducted using zebrafish embryos. The optimized formulation (F1), prepared with Eudragit RLPO, showed a drug content of 96.68%, entrapment efficiency of 87.5%, particle size of 310.7 nm, PDI of 0.212, and a zeta potential of + 25.7 mV. It achieved 93.93% cumulative drug release sustained up to 8 h. SEM revealed spherical morphology, while DSC and XRD confirmed retention of the crystalline nature of gliclazide. FT-IR analysis showed no significant drug-excipient interaction. Toxicity studies in zebrafish embryos indicated no significant toxic effects. The developed formulation demonstrated superior safety and efficacy compared to the marketed formulation. The study successfully demonstrated that GLNPs offer a promising alternative for enhancing the oral bioavailability of gliclazide with improved safety and sustained therapeutic efficacy in a zebrafish model.

Graphical Abstract

Formulation, characterization, antidiabetic evaluation, and toxicity study on zebrafish of gliclazide loaded polymeric nanoparticles