Design and evaluation of glimepiride hydrogel for transdermal delivery

Abstract

The solubility of glimepiride (GM) was improved from 1.6 μg/mL to 22.0 mg/mL when GM and meglumine (MU) complexes were prepared. Therefore, transdermal hydrogels of GM Carbopol (GM-CP) and GM hydroxypropyl methylcellulose pullulan (GM-HPMC-Pu) were prepared successfully utilizing the improved drug solubility by GM-MU. Based on a single factor experiment and response surface methodology, two kinds of hydrogel formulations were optimized by drug release studies in vitro. The optimized GM-CP hydrogel was composed of GM, a mixture of azone and oleic acid (1:1, 2.6%, v/v) and carbopol 940 (1%, w/v). The GM-HPMC-Pu hydrogel was developed using GM, HPMC (3.5%, w/v), Pu (1.5%, w/v), glycerol (5%, v/v), azone (2.9%, v/v) and oleic acid (2.6%, v/v). The study of hydrogels in vivo was performed using rabbits. The results indicated that the drug could sustain release from GM-CP or GM-HPMC-Pu hydrogel and maintain the high plasma concentration for 48 h. Compared with commercial GM tablets, the relative bioavailability of GM-CP and GM-HPMC-Pu hydrogel reached 48% and 133%, respectively. Moreover, the drug release in vitro could well predict its absorption in vivo. There was a good correlation (R²≥0.966) in GM hydrogel between the drug release in vitro and transdermal absorption in vivo. Therefore, a novel GM hydrogel dosage form may be considered to design.

Keywords:

• Glimepiride
• meglumine
• hydrogel
• bioavailability
• in vitro-in vivo correlation

Disclosure statement

The authors declare no competing interest.

Additional information

Funding

This work was supported by the Natural Science Foundation of Hebei Province (No. C2021201026) and the Science and Technology Research Projects in Colleges and Universities of Hebei Province (ZD2016102).