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<p>Effective diabetes management necessitates innovative strategies that simultaneously stimulate β-cell growth and prevent apoptosis. While sitagliptin is an established therapeutic, its clinical utility is often hampered by suboptimal oral bioavailability and a lack of site-specific delivery. This research details the development and <i>in vitro</i> assessment of Sita-Ex-Cs-SeNPs, a subcutaneous nanocarrier composed of sitagliptin-loaded chitosan-selenium nanoparticles conjugated with exenatide. The platform is engineered to leverage GLP-1 receptor affinity for pancreatic targeting and utilize selenium’s intrinsic antioxidant properties to achieve therapeutic synergy. We employed the ionotropic gelation technique to encapsulate sitagliptin and integrate exenatide and selenium into a unified, stable delivery system. The resulting nanoparticles exhibited a spherical architecture with an average diameter of 314.1 nm and a zeta potential of + 18.7 mV. We achieved a high encapsulation efficiency of 98%. Analytical techniques (DSC and PXRD) confirmed that sitagliptin transitioned to an amorphous state, while FTIR validated successful peptide conjugation. Release kinetics followed the Weibull model, demonstrating a controlled biphasic profile (57% over 24 h) that significantly extends the therapeutic window compared to the free drug. <i>Sita-Ex-Cs-SeNPs</i> offer a promising, biocompatible approach for targeted diabetes intervention. Although <i>in vitro</i> results confirm stable sustained release, subsequent <i>in vivo</i> trials are essential to validate their efficacy in β-cell preservation.</p> Graphical Abstract <p></p>

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The Preparation and Physicochemical Characterization of a Triple Synergistic Nanoplatform Designed for Targeted Subcutaneous Delivery of Sitagliptin with Potential for β-Cell Preservation

  • 期刊论文

  • 发表日期：

    2026年7月2日

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  • Mo’tasem M. Alsmadi,
  • Rana Obaidat

摘要

Effective diabetes management necessitates innovative strategies that simultaneously stimulate β-cell growth and prevent apoptosis. While sitagliptin is an established therapeutic, its clinical utility is often hampered by suboptimal oral bioavailability and a lack of site-specific delivery. This research details the development and in vitro assessment of Sita-Ex-Cs-SeNPs, a subcutaneous nanocarrier composed of sitagliptin-loaded chitosan-selenium nanoparticles conjugated with exenatide. The platform is engineered to leverage GLP-1 receptor affinity for pancreatic targeting and utilize selenium’s intrinsic antioxidant properties to achieve therapeutic synergy. We employed the ionotropic gelation technique to encapsulate sitagliptin and integrate exenatide and selenium into a unified, stable delivery system. The resulting nanoparticles exhibited a spherical architecture with an average diameter of 314.1 nm and a zeta potential of + 18.7 mV. We achieved a high encapsulation efficiency of 98%. Analytical techniques (DSC and PXRD) confirmed that sitagliptin transitioned to an amorphous state, while FTIR validated successful peptide conjugation. Release kinetics followed the Weibull model, demonstrating a controlled biphasic profile (57% over 24 h) that significantly extends the therapeutic window compared to the free drug. Sita-Ex-Cs-SeNPs offer a promising, biocompatible approach for targeted diabetes intervention. Although in vitro results confirm stable sustained release, subsequent in vivo trials are essential to validate their efficacy in β-cell preservation.

Graphical Abstract