Topikal administration av VR1 antagonist aktiv i människa - en möjlighet att behandla neuropatisk smärta

Purpose and goal

The aim was to develop a topical formulation for a VR1 antagonist active in human with the opportunity to manage neuropathic pain. The work within the project has confirmed promising solubility, permeability and flux (rate) in suitable excipients. Furthermore, the flux for the substance has even been improved in combination with gelifying components. The project has a formulation suitable for topical safety and concept study in man.

Expected results and effects

Solubility data generated for a battery of excipients cretaed the basis to choose excipients to be tested in permeability studies. The flux determined in Frans Cell system for the substance was demonstrated to be moderate in all three components. The combination of gelcomponents with the excipients even increase the flux further for the substance 5 times. This formulation will be used in the topical safety study in rabbit and in the clinical concept study.

Planned approach and implementation

Solubilities was tested in a battery of excipients of which three were selected for the permeability studies. Permeability test was performed using Franz Cell system and high permeable caffeine as reference compound and positive control. The flux was further tested for two of the excipients in combination with gel components which increases the viscosity and allow use in toxicity and clinical studies.