Scholarlink

Purpose <p>Dipeptidyl peptidase-4 (DPP-4) inhibitors, such as vildagliptin, commonly utilized in the management of type 2 diabetes mellitus, have good aqueous solubility and oral bioavailability but its short half-life requires frequent dosing, posing significant challenges in drug administration. Proliposomes are promising provesicular lipid-based carriers that can modulate drug release and improve formulation stability. This study focuses on developing proliposomes for sustained release rather than permeability enhancement.</p> Methods <p>Vildagliptin-encapsulated proliposomes (PLs) were synthesized utilizing a modified slurry technique. The formulations were assessed for micromeritic characteristics, encapsulation efficiency, vesicle dimensions, zeta potential, and in-vitro drug release kinetics.</p> Results <p>The prepared PLs exhibited good flow properties with Carr’s index ranging from 6.67% to 19.3%. Entrapment efficiency ranged from 65.55% to 86.68%. The optimized formulation (VLG-5) showed a particle size of 385 ± 5&#xa0;nm, PDI of 0.31 ± 0.06, and zeta potential of − 16.9 ± 2.0 mV, indicating acceptable vesicular characteristics. In-vitro release studies demonstrated sustained drug release up to 24&#xa0;h (&gt; 94%).</p> Conclusion <p>The developed proliposomal system successfully provided sustained release of Vildagliptin. However, further <i>in -vivo</i> studies are required to establish its pharmacokinetic and therapeutic advantages.</p> Graphical Abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Development and Characterization of Proliposomes for Sustained Oral Delivery of the DPP-4 Inhibitor Vildagliptin

  • 期刊论文

  • 发表日期：

    2026年4月28日

查看全文
  • Shazia Ashraf,
  • Asadullah Madni,
  • Faizan Akram,
  • Muhammad Farhan Hanif,
  • Afifa Shafiq,
  • Iqra Fatima Ayub

摘要

Purpose

Dipeptidyl peptidase-4 (DPP-4) inhibitors, such as vildagliptin, commonly utilized in the management of type 2 diabetes mellitus, have good aqueous solubility and oral bioavailability but its short half-life requires frequent dosing, posing significant challenges in drug administration. Proliposomes are promising provesicular lipid-based carriers that can modulate drug release and improve formulation stability. This study focuses on developing proliposomes for sustained release rather than permeability enhancement.

Methods

Vildagliptin-encapsulated proliposomes (PLs) were synthesized utilizing a modified slurry technique. The formulations were assessed for micromeritic characteristics, encapsulation efficiency, vesicle dimensions, zeta potential, and in-vitro drug release kinetics.

Results

The prepared PLs exhibited good flow properties with Carr’s index ranging from 6.67% to 19.3%. Entrapment efficiency ranged from 65.55% to 86.68%. The optimized formulation (VLG-5) showed a particle size of 385 ± 5 nm, PDI of 0.31 ± 0.06, and zeta potential of − 16.9 ± 2.0 mV, indicating acceptable vesicular characteristics. In-vitro release studies demonstrated sustained drug release up to 24 h (> 94%).

Conclusion

The developed proliposomal system successfully provided sustained release of Vildagliptin. However, further in -vivo studies are required to establish its pharmacokinetic and therapeutic advantages.

Graphical Abstract