Extrudates of lipophilic tetracycline complexes: A new option for periodontitis therapy.

Kirchberg, Martin; Eick, Sigrun; Buchholz, Mirko; Kiesow, Andreas; Sarembe, Sandra; Mäder, Karsten (2019). Extrudates of lipophilic tetracycline complexes: A new option for periodontitis therapy. International journal of pharmaceutics, 572, p. 118794. Elsevier 10.1016/j.ijpharm.2019.118794

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The objective of this study was to develop an improved drug delivery system for the local antimicrobial treatment of periodontitis, that offers enhanced drug stability, easy application and controlled release over several weeks. Chelate complexes consisting of a tetracycline antibiotic and a fatty acid salt were developed. Minocycline and doxycycline were paired with magnesium- and calcium stearate in different molar ratios. These chelate complexes stabilize the active pharmaceutical ingredient and enable the incorporation into a PLGA (poly(lactic-co-glycolic acid)) polymer matrix via hot melt extrusion. The chelate complexes were characterized via UV/Vis- and IR-spectroscopy. A high antibiotic activity of the complex was observed in a disc diffusion test. The drug complex was mixed with different PLGA-polymers and cryomilled in advance of the extrusion. The hot melt extrusion yielded homogeneous extrudates with a diameter from 600 to 900 µm. They contain 11.5% of minocycline, are adjustable in length and are easy to handle. In vitro release studies revealed a controlled release of the drug over 42 days. In conclusion, the developed extrudates are promising systems to improve the treatment of periodontitis.

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