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<p>The rapidly expanding subject of nanotechnology is led by solid lipid nanoparticles (SLNs), which have several potential uses in research and medicine delivery. For improving the oral bioavailability of medications with limited water solubility, these techniques are far superior to conventional ones. The basic goal of our experiment was to develop and assess pioglitazone-loaded SLNs for improving the bioavailability. Glyceryl monostearate, as a solid lipid and Tween 80, as a surfactant, are the main components of the formulated SLNs. By using the solvent injection approach, pioglitazone-loaded SLNs were created. Using a Zetasizer, the mean particle sizes and zeta potential were calculated at a temperature of 25&#xa0;°C. Scanning electron microscopy was used to analyze the morphology of nanoparticles. An X-ray diffractometer was used to assess the pioglitazone, PGL-SLN’s crystallinity. The lyophilized F2 SLNs preparation was amassed in a vial for 90&#xa0;days at the condition of 40 ± 2&#xa0;°C/75 ± 5%. Initially, 0.2&#xa0;µml of streptozotocin (STZ) was induced in the zebrafish to induce diabetes. After different characterization process, the formulation was analyzed for in vivo and in vitro study. The optimized formulation (F2) had an encapsulation efficiency of 85.8%, particle size 149&#xa0;nm, PDI 0.091, and a zeta potential − 3.66&#xa0;mv. The cumulative percentage drug release of the optimized formulation (F2) shows 51.6% for 10&#xa0;h which shows sustained release and no significant toxicity is present in the pioglitazone-loaded SLNs. Pioglitazone-loaded lipid nanoparticles were given to diabetic zebrafish to assess their effectiveness. The blood glucose levels of diabetic fish have decreased after pharmacological therapy on the appropriate day. All zebrafish embryos exposed to methanol extract were evaluated for teratogenicity. The synthesized SLNs had a uniform dispersion of nanoparticles and a spherical shape. Extended drug release was demonstrated by pioglitazone-loaded SLNs, which fitted to a first-order model. When fed an optimum formulation, diabetic zebrafish demonstrated a decrease in blood glucose levels on the appropriate day. Furthermore, as there was no toxicity discovered, the zebrafish embryos treated with pioglitazone-SLNs were healthy and developing normally.</p> Graphical Abstract <p></p>

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Design and Optimization of a Model Bcs Class II Drug-Loaded Glyceryl Monostearate Nanoparticles: Antidiabetic Efficacy and Teratogenic Safety in Zebrafish

  • 期刊论文

  • 发表日期：

    2025年8月11日

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  • Swarupananda Mukherjee,
  • Avinaba Das,
  • Dipanjan Karati,
  • Dibya Sinha,
  • Mainak Chakraborty,
  • Prabhat Kr Mishra,
  • Mohammed Gulzar Ahmed

摘要

The rapidly expanding subject of nanotechnology is led by solid lipid nanoparticles (SLNs), which have several potential uses in research and medicine delivery. For improving the oral bioavailability of medications with limited water solubility, these techniques are far superior to conventional ones. The basic goal of our experiment was to develop and assess pioglitazone-loaded SLNs for improving the bioavailability. Glyceryl monostearate, as a solid lipid and Tween 80, as a surfactant, are the main components of the formulated SLNs. By using the solvent injection approach, pioglitazone-loaded SLNs were created. Using a Zetasizer, the mean particle sizes and zeta potential were calculated at a temperature of 25 °C. Scanning electron microscopy was used to analyze the morphology of nanoparticles. An X-ray diffractometer was used to assess the pioglitazone, PGL-SLN’s crystallinity. The lyophilized F2 SLNs preparation was amassed in a vial for 90 days at the condition of 40 ± 2 °C/75 ± 5%. Initially, 0.2 µml of streptozotocin (STZ) was induced in the zebrafish to induce diabetes. After different characterization process, the formulation was analyzed for in vivo and in vitro study. The optimized formulation (F2) had an encapsulation efficiency of 85.8%, particle size 149 nm, PDI 0.091, and a zeta potential − 3.66 mv. The cumulative percentage drug release of the optimized formulation (F2) shows 51.6% for 10 h which shows sustained release and no significant toxicity is present in the pioglitazone-loaded SLNs. Pioglitazone-loaded lipid nanoparticles were given to diabetic zebrafish to assess their effectiveness. The blood glucose levels of diabetic fish have decreased after pharmacological therapy on the appropriate day. All zebrafish embryos exposed to methanol extract were evaluated for teratogenicity. The synthesized SLNs had a uniform dispersion of nanoparticles and a spherical shape. Extended drug release was demonstrated by pioglitazone-loaded SLNs, which fitted to a first-order model. When fed an optimum formulation, diabetic zebrafish demonstrated a decrease in blood glucose levels on the appropriate day. Furthermore, as there was no toxicity discovered, the zebrafish embryos treated with pioglitazone-SLNs were healthy and developing normally.

Graphical Abstract