Beyer, SusanneSusanneBeyerMoosmann, AlineAlineMoosmannKahnt, Astrid S.Astrid S.KahntUlshöfer, ThomasThomasUlshöferParnham, Michael J.Michael J.ParnhamFerreirós, NereaNereaFerreirósWagner, SylviaSylviaWagnerWacker, Matthias G.Matthias G.Wacker2022-03-052022-03-052015https://publica.fraunhofer.de/handle/publica/24142010.1007/s11095-015-1759-2Purpose The contribution of permeability and drug release to drug targeting were investigated in the course of development of a nanosized formulation of the anti-inflammatory compound TMP-001, for the local treatment in the gastrointestinal tract. Methods TMP-001 was encapsulated by nanoprecipitation into Eudragit® RS 100. The permeability of these carriers was investigated in an Ussing chamber model and the release rate was determined under biorelevant conditions. Formulation toxicity and particle-cell-interaction were investigated by flow cytometry, fluorescence and electron microscopy. Furthermore, spray drying was performed. Results Effective internalization of Eudragit®-nanoparticles into cancer cells was demonstrated. A burst release of the nanoparticles implied poor interaction of TMP-001 with Eudragit®. A sustained release (70.5% release after 30 min compared to 98.0% for the API) was accomplished after spray drying yielded an increased particle size. Recovery rate of TMP-001 after spray drying was 94.2 ± 5.9%. Conclusion The release of API from polymeric nanoparticles contributes profoundly to the in vivo-performance of drug delivery devices in the gastrointestinal tract. The impact of drug-polymer interaction and particle size was analyzed. Sustained release of TMP-001 could only be achieved by increasing particle size. Therefore, biorelevant release testing has been demonstrated to be a valid tool for nanoformulation design.en540615571572journal article