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Objective <p>The objective of the present investigation was to preparesolid lipid nanoparticles of the BCS class II drug Glimepiride (GP) comprising coconut oil and Poloxamer 407, for improving the in vitro dissolution profile of the drug.Additionally, formulations were statistically optimized (3<sup>2</sup> full factorial experimental design) for focusing on the impact of independent variables on dependent factors of the nanoformulation (particle size, encapsulation efficiency, and drug content) through response surface methodology.</p> Significance <p>Orally given lipophilic drug moieties, especially those in the BCS class II and IV categories, may have a number of issues that lead to poor absorption, bioavailability, and significant intra-and inter-subject variance.A biocompatible colloidal lipidic nanocarrier, solid lipid nanoparticles, are considered as potent substitute against traditional polymeric nanocarriers for delivering BCS class II and IV categories of drugs.</p> Methods <p>Glimepiride solid lipid nanoparticles was prepared by solvent evaporation method and then physico-chemical parameters, thermal analysis, X-ray diffraction (XRD) and scanning electron microscopy (SEM) analysis, and stability profile of the formulations were assessed.</p> Results <p>The optimized Glimepiride SLNsdemonstrated particle size of 329.58 ± 0.63&#xa0;nm, significant encapsulation efficiency (91.41 ± 0.13%), maximum GP content (88.16 ± 1.17%) with the percentage bias of 0.13–0.95 between observed and predicted data. The dose dependent ability of optimized formulation to reduce HEK293 cell viability and potential streptozotocin induced in vivo anti-diabetic response in terms of satisfactory oral glucose tolerance level, concentration of liver enzymes, and lipid profiles without organ toxicity confirming from histopathological analysis was stated the GP-loaded SLNs as potent candidate for diabetes treatment.</p> Conclusion <p>The optimized SLNs formulation has admirable good drug release property. Furthermore, the optimized formulation revealed dose dependent cytotoxicity on cell lines with satisfactory in vivo anti-diabetic activities.</p> Graphical Abstract <p></p>

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Design and Optimization of Glimepiride Loaded Lipid Nanocarriers: Characterization and In vivo Evaluation

  • 期刊论文

  • 发表日期：

    2026年5月14日

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  • Swarupananda Mukherjee,
  • Saheli Naskar,
  • Priya Ghosh,
  • Sakuntala Gayen,
  • Souvik Roy,
  • Soumendra Nath Bandyopadhyay,
  • Pasquale De Toro,
  • Ayon Dutta,
  • Dipanjan Karati,
  • Dipanjana Ash

摘要

Objective

The objective of the present investigation was to preparesolid lipid nanoparticles of the BCS class II drug Glimepiride (GP) comprising coconut oil and Poloxamer 407, for improving the in vitro dissolution profile of the drug.Additionally, formulations were statistically optimized (32 full factorial experimental design) for focusing on the impact of independent variables on dependent factors of the nanoformulation (particle size, encapsulation efficiency, and drug content) through response surface methodology.

Significance

Orally given lipophilic drug moieties, especially those in the BCS class II and IV categories, may have a number of issues that lead to poor absorption, bioavailability, and significant intra-and inter-subject variance.A biocompatible colloidal lipidic nanocarrier, solid lipid nanoparticles, are considered as potent substitute against traditional polymeric nanocarriers for delivering BCS class II and IV categories of drugs.

Methods

Glimepiride solid lipid nanoparticles was prepared by solvent evaporation method and then physico-chemical parameters, thermal analysis, X-ray diffraction (XRD) and scanning electron microscopy (SEM) analysis, and stability profile of the formulations were assessed.

Results

The optimized Glimepiride SLNsdemonstrated particle size of 329.58 ± 0.63 nm, significant encapsulation efficiency (91.41 ± 0.13%), maximum GP content (88.16 ± 1.17%) with the percentage bias of 0.13–0.95 between observed and predicted data. The dose dependent ability of optimized formulation to reduce HEK293 cell viability and potential streptozotocin induced in vivo anti-diabetic response in terms of satisfactory oral glucose tolerance level, concentration of liver enzymes, and lipid profiles without organ toxicity confirming from histopathological analysis was stated the GP-loaded SLNs as potent candidate for diabetes treatment.

Conclusion

The optimized SLNs formulation has admirable good drug release property. Furthermore, the optimized formulation revealed dose dependent cytotoxicity on cell lines with satisfactory in vivo anti-diabetic activities.

Graphical Abstract