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Drug release and targeting: The versatility of polymethacrylate nanoparticles for peroral administration revealed by using an optimized Iin Vitro-toolbox

: Beyer, Susanne; Moosmann, Aline; Kahnt, Astrid S.; Ulshöfer, Thomas; Parnham, Michael J.; Ferreirós, Nerea; Wagner, Sylvia; Wacker, Matthias G.


Pharmaceutical research 32 (2015), No.12, pp.3986-3998
ISSN: 0724-8741
ISSN: 0739-0742
Journal Article
Fraunhofer IBMT ()

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.
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.
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%.
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.