Fabrication of prostructured spanlastics gel for improving transdermal effect of dapagliflozin: In vitro characterization studies and in vivo antidiabetic activity

• Published in: Journal of drug delivery science and technology 2024-08, Vol.97, p.105804, Article 105804
• Main Authors: Barakat, Elsaied H., Kassem, Abdulsalam M., Ibrahim, Mohamed F., Elsayad, Maged K., Abdelgawad, Wedian Younis, Salama, Ayman, Alruwaili, Nabil K., Alsaidan, Omar Awad, Elmowafy, Mohammed
• Format: Article
• Language: English
• Subjects: Antidiabetic activity; Dapagliflozin; Skin permeation; Spanlastic gel; Spanlastic vesicles
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2024.105804

Dapagliflozin is a recently approved glucose-lowering agent for the management of type II diabetes mellitus. Low solubility and stability lead to its poor oral bioavailability. Prostructured spanlastic gel is very less hydrated preform of spanlastic vesicles. Therefore, the aim of this study was to explore the potential of prostructured spanlastic gel for enhancing both drug stability and transdermal delivery. The prostructured spanlastic gel formulations were fabricated by coacervation phase separation method, using Span 60 together with Tween 80 or Myrj 52 as an edge activator. Formulations were characterized for drug content, in vitro release and ex vivo skin permeability. Verification of vesicular form was assessed by hydration and the resultant formulations were characterized. Selected formulations were assessed for morphology, interaction of drug with other components, stability and antidiabetic activity. Drug content percentage of spanlastic gels was found to be in range 98.1 ± 1.9 to 94.2 ± 2.0 %. Significant (p