Formulation, characterization and optimization of a topical gel containing tranexamic acid to prevent superficial bleeding: In vivo and in vitro evaluations

INTRODUCTION: Tranexamic acid (TXA) is used systemically to stop bleeding, but it can lead to thromboembolism. Trials showed the efficacy of topical TXA on local hemorrhages. However, there is a need for an efficient delivery system that can keep the drug at the site of action
METHODS: To develop a gel containing TXA 3% optimized in terms of viscosity and dispersibility, the Central Composite Design (CCD) based on two factors-three levels (Carbopol 940 and HPMC, 1-1.5% and 1-2% respectively) was applied. The spreadability and viscosity were assessed using the glass slide and rheometer, respectively. To confirm the compatibility of TXA with gel, FTIR spectroscopy was performed. Drug content uniformity was analyzed by a spectroscopy method. An ex vivo mice model, using Franz cells was applied to evaluate the permeation of TXA through the skin. To investigate the effect of topical TXA gel on bleeding time, the IVY human method was performed.

RESULTS: Results: HPMC/carbopol 940 (1: 1w/w) gel has shown the highest quality in terms of viscosity and dispersibility (3.982 ± 17.6 and 6.052 ± 3562 respectively). The FTIR absorption spectrum showed that all of the TXA index peaks appeared without displacement. The complete encapsulated TXA content was uniformly dispersed throughout the gel. In vitro TXA cumulative release reached 90% in 4 hours. In vivo, the bleeding time for the TXA gel was significantly lower than the TXA solution and control.


DISCUSSION AND CONCLUSION: The results confirm the importance of further studies on this formulation as a potential medication to stop acute superficial bleeding.