BrainDos™ formulation increases the anti-inflammatory activity by almost 2-fold after 4h
Il-6 pro-inflammatory cytokine over 80% reduced with BrainDos™ technology
MetP Pharma AG, leveraging the proprietary nose-to-brain drug delivery technology BrainDos™ in internal and external product development and manufacturing programs, today announced preclinical data showing that tirzepatide in a BrainDos™ formulation reduced pro-inflammatory cytokine Il-6 by more than 80% and 2-fold stronger than with aqueous tirzepatide solution. The full effect of the IL-6 reduction with tirzepatide/BrainDos™ formulation was reached after 4 hours.
MetP Pharma investigated the anti-inflammatory effect of tirzepatide in SH-SY5Y neuroblastoma cell line. The cells were first treated with lipopolysaccharide (LPS) to induce inflammation. After 24 hours exposure to LPS, the cells were treated either with tirzepatide in a BrainDos™ formulation or aqueous tirzepatide solution (phosphate-buffered saline). The aqueous tirzepatide solution was similar to Lilly’s Mounjaro® only slightly differing in the salt composition. The anti-inflammatory effect was determined by measuring interleukine IL-6 reduction.
The tirzepatide/BrainDos™ formulation reduced IL-6 levels after 4 hours treatment by 87.9% versus a 44.6% reduction with tirzepatide solution. The anti-inflammatory effect of tirzepatide/BrainDos™ formulation was nearly complete after 4 hours treatment while with tirzepatide solution the effect was more pronounced after 24 hours treatment (44.6% versus 58.6%). The data demonstrate that the BrainDos™ formulation increases the anti-inflammatory activity by almost 2-fold at 4 hours, and 1.5- fold at 24 hours where it also shows a lasting effect exceeding the effect of the tirzepatide solution. The tirzepatide concentration in both the BrainDos™ formulation and the aqueous solution was 10nM.
IL-6 response after 4 h drug treatment IL-6 response after 24 h drug treatment
Tirzepatide is a synthetic, dual GIP/GLP-1 receptor agonist that mimics the two hormones naturally produced by the gut and the brain. It is believed that their effect on the central nervous system reduces the feeling of hunger. Due to their charge, these peptide molecules do not pass the blood-brain barrier to a sufficient extent or not at all. BrainDos™ formulation is a potent nose-to-brain drug delivery technology developed to bypasses the blood-brain barrier.
Dr. Claudia Mattern, Chief Scientific Officer at MetP Pharma says: “BrainDos™ formulated tirzepatide is a potent anti-inflammatory agent outperforming the aqueous tirzepatide solution in reducing IL-6 levels. We believe that the BrainDos™ technology has the potential to increase the anti-inflammatory effect of weight-loss products such as Wegovy® and Mounjaro®.”
Recently, MetP Pharma announced preclinical results showing that GLP-1 receptor agonist semaglutide formulated with the BrainDos™ technology significantly increases drug delivery into cells (1). Chronic brain inflammation is involved in the etiopathology of many neurodegenerative diseases (2) and innovative formulations such as with BrainDos™ technology could have a broad clinical potential far beyond managing obesity.
About BrainDos™
BrainDos™ is an intranasal oil-based drug delivery system developed to bypasses the blood-brain barrier (BBB) and allowing precise drug administration. BrainDos™ consists of a thixotropic oleogel, Silcum®, enclosed in a mono-dose applicator (Lecticula®). The advanced gel system incorporates the active pharmaceutical ingredient (API) within a lipid-based matrix and exhibits distinctive intranasal drug retention and mucosal adhesion properties thus allowing optimal drug release and exposure to the nasal mucosa. Silcum® facilitates the direct entry of drugs to the brain via the olfactory and trigeminal pathw...
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