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Novel polymeric micelles for drug delivery: Material characterization and formulation screening

: Janas, C.; Mostaphaoui, Z.; Schmiederer, L.; Bauer, J.; Wacker, M.G.


International Journal of Pharmaceutics 509 (2016), Nr.1-2, S.197-207
ISSN: 0378-5173
Fraunhofer IME ()

A rising number of new chemical entities that exhibit only poor aqueous solubility are identified in drug discovery processes. Polymeric micelles composed of block copolymers (BP) facilitate the delivery of such lipophilic molecules in drug therapy. Consequently, a rational screening and selection procedure for novel BP was established. Further, the interplay of polymer structure, micelle formation and drug binding was studied. Therefore seven polymers (BP001 to BP007) were synthesized from different monomer compositions resulting in nanocarriers varying in surface decoration and lipophilicity. These polymers were characterized by H1-NMR and SEC. The molecular weight was ranging between 13 and 37 kDa. The critical micelle concentration and micellar integrity in presence of human plasma were determined. Micelles were loaded with dexamethasone and characterized with regards to their size, morphology and surface charge. Polymeric micelles with a size of 49.21-236.37 nm were obtained.