Glucagon-like peptide-1 (GLP-1) Receptor Agonist Semaglutide in an Oleogel Formulation Using the BrainDos Technology Significantly Increases Drug Delivery into Cells
May 8, 2024 – Drug Delivery, Pharmaceutical – MetP Pharma, blood-brain barrier, drug delivery, obesity
- Semaglutide is the active ingredient of weight loss medications Ozempic and Wegovy
- Semaglutide as an oleogel formulation using the BrainDos technology is internalised much more strongly than in an aqueous formulation used for example in pens
- This new formulation and intra-nasal application could help alleviate the obesity-related healthcare burden as the application costs are significantly lower than with pens.
8 May 2024 — Emmetten, Switzerland — MetP Pharma, leveraging the proprietary nose-to-brain drug delivery technology BrainDos in internal and external product development and manufacturing programmes, today announced promising preclinical research results that strongly support the further development of semaglutide in an oleogel formulation using the BrainDos drug delivery technology.
Semaglutide, the active ingredient of Ozempic and Wegovy, is an antidiabetic medication used for the treatment of type 2 diabetes as well as an anti-obesity medication used for long-term weight management. It is a Glucagon-Like Peptide-1 Receptor Agonist (GLP-1-RA) that is currently administered through subcutaneous injection using pens.
GLP-1 receptors are found on beta cells of the pancreas and on neurons of the brain. There, signal chains are activated that suppress the feeling of hunger and increase the feeling of satiety. It is proven that GLP-1 RAs can send information to the brain via neural and humoral pathways.
Preclinical studies in Cultured Human Airway Epithelial Cells (Calu-3) conducted at MetP Pharma demonstrate that the semaglutide oleogel in the BrainDos formulation leads to a 10-fold increase in tyrosine hydroxylase (TH) expression, compared to only a 2-fold increase of the aqueous semaglutide solution as used for example in pens. As obesity leads to a reduction in tyrosine hydroxylase (TH) levels an increase in TH levels is a suitable biomarker for drug delivery. The results also demonstrate a significantly higher TH response at 4h than at 24h post treatment but the TH level at 24h is still about 3-fold higher than the untreated control demonstrating consistent activity. The semaglutide concentration in both the oleogel formulation and the aqueous solution was 10nM.
Dr Claudia Mattern, chief scientific officer at MetP Pharma, says: “The preclinical studies clearly show that the oleogel formulation with BrainDos increases the delivery of semaglutide into cells. This makes BrainDos suitable for re-formulating active ingredients with expiring patents and re-patenting them using a new, innovative application method. It is important to understand that BrainDos is an innovative nose-to-brain drug delivery technology that in no way is comparable to traditional nasal sprays.”
A nasal application of semaglutide could have several advantages compared to pens such as non-invasiveness, fast and easy administration, painless application for patients with needle phobia, fewer adverse events through reduced systemic exposure of the drug and much less costs per application than pens. In addition, there is the ability for direct CNS delivery using BrainDos potentially resulting in a higher bioavailability.
Obesity is a huge problem in many countries and is even classified as an epidemic by the World Health Organization (WHO). This new formulation and administration mode could help alleviate the obesity-related healthcare problem as the manufacturing costs are significantly lower than with the currently used pens and the application is more convenient.
About MetP Pharma AG
MetP Pharma is an independent, specialised pharmaceutical R&D and product development company based in Switzerland. The company has developed BrainDos, an advanced and comprehensively patented nose-to-brain drug delivery system allowing to bypass the blood-brain barrier. The brain targeting effect of BrainDos has been demonstrated through various proof-of-concept studies. BrainDos is a fully developed and flexible technology platform that is significantly reducing the risk of pharmaceutical product development. The company’s internal product development programme includes intranasal products for the indications concussion, insomnia, attention deficit hyperactivity disorder (ADHD), multiple sclerosis (MS) and hypogonadism. MetP also provides pharmaceutical development services based on its proprietary and worldwide patented intranasal BrainDos delivery technology. The company’s research has been published in 65 peer-reviewed journals and a robust intellectual property portfolio exists in a large number of countries until 2037/2039. Visit: mattern-pharma.com.
