Active ingredients for the oral cavity: From a tablet to a locally effective gel

Applying medical or cosmetic active ingredients in just the right place inside the oral cavity continues to present a major challenge. This is partly because many medications do not remain in the mouth for long enough due to salivation. As a result, medications for some symptoms must be used systemically, i.e. to the whole body, instead of locally. This is particularly true for periodontitis – one of the world’s most common infections, which not only leads to the destruction of the periodontium, but also increases the risk of rheumatoid arthritis, diabetes, and cardiovascular disease. Alongside mechanical removal of the microbial covering for periodontitis, broad-spectrum antibiotics must also be administered in tablet form as a supportive treatment. The high doses required here cause side effects, such as a change in and decimation of the intestinal flora as well as promoting the development of resistance, which represent an ever greater problem in everyday clinical practice in industrialized and newly industrialized countries.

Wirkstoff Mundraum Gel Parodontitis
© MEV-Verlag
A local active ingredient for the oral cavity was developed at Fraunhofer IMWS.

The researchers at the Fraunhofer Institute for Microstructure of Materials and Systems IMWS are thus working together with the Fraunhofer Institute for Cell Therapy and Immunology IZI in Halle (Saale) on a form of application that is intended to avoid this kind of systemic approach. The aim is to develop a corresponding antibiotic or antiseptic that can be placed locally as easily and pain-free as possible. At the same time, the required effective level of the medication must be maintained over a long period of time.

First of all, a new formulation platform is being developed and tested with the help of an active ingredient that is already known and used for periodontitis. It is a kind of mode of transport for the active ingredient that enables long-lasting local release. This platform is intended to then be expanded to a wide range of substances and purposes later on. Subsequent use in preventative or selective antiseptic oral care products is being considered.

»Our task in the project is to analyze the properties of developed active ingredients. We create various test models to test the interaction with the hard and soft tissue in conditions that are as real as possible in the oral cavity. It is important to investigate the adhesion, wetting, and rheological properties of the formulations,« explains Dr. Andreas Kiesow, head of the ‘Characterization of Medical and Cosmetic Care Products’ working group at Fraunhofer IMWS in Halle (Saale).

»During this project, we are investigating, among other things, the release of the active ingredient from the dosage form under strictly regulated conditions to thus ensure the subsequent long-lasting local effect in the oral cavity,« adds Dr. Mirko Buchholz, head of the ‘Drug Design and Analytical Chemistry’ working group at Fraunhofer IZI-MWT in Halle (Saale).

The project runs until June 30, 2019. It is undertaken in close collaboration between the Fraunhofer Institute for Microstructure of Materials and Systems IMWS and the Fraunhofer Institute for Cell Therapy and Immunology IZI, the Active Ingredient Biochemistry and Treatment Development project group IZI-MWT, and the High-Performance Center for Chemistry and Biosystems Technology founded in Halle (Saale) in the summer. Experts in the field of pharmaceutical technology (Institute of Pharmacy, Martin Luther University Halle-Wittenberg) and from dentistry (Dentistry Clinks, University of Bern) are closely involved in the development work right from the start as professional partners for practical problems from a dentist’s and patient’s viewpoint. What’s more, Pharmazeutische Kontroll- und Herstellungslabor GmbH, mibe GmbH Arzneimittel, and Skinomics GmbH are also contributing their professional expertise.