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Traub-Hoffmann, Kerstin; Gegenfurtner, Katrin; Kraft, Kay-Uwe; Friess, Wolfgang (2020): Spray congealed solid lipid microparticles as a sustained release delivery system for Gonadorelin [6-D-Phe]: Production, optimization and in vitro release behavior. In: European Journal of Pharmaceutics and Biopharmaceutics, Vol. 154: pp. 18-32
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Abstract

Sustained release lipid microparticles for a potential veterinary application were produced by the means of spray congealing using saturated triglycerides with respective surfactants. The spray congealing process was optimized using unloaded and loaded microparticles, revealing the highest impact of the spray flow on material loss. Yield could be optimized by increasing the spray flow as well as a reduction of the melt temperature from 90 to 75 degrees C. For the delivery system developed in this study, a release of around 15 days was targeted. The release profile was in first hand determined with the use of model substances (aspartame and tryptophan), before incorporating the decapeptide Gonadorelin [6-D-Phe]. Release could be controlled between 2 and 28 d, which was dependent on stability of microparticles upon incubation, type and concentration of emulsifier, as well as the used triglyceride. Differential scanning calorimetry and X-ray powder diffraction confirmed the crystallization behavior of C14 and C16-triglycerides in combination with various emulsifiers in different modification without impact on release.