HPMA based amphiphilic copolymers mediate central nervous effects of domperidone.

Mirjam Hemmelmann, Christiane Knoth, Ulrich Schmitt, Mareli Allmeroth, Dorothea Moderegger, Matthias Barz, Kaloian Koynov, Christoph Hiemke, Frank Rösch, Rudolf Zentel

Index: Macromol. Rapid Commun. 32(9-10) , 712-7, (2011)

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Abstract

In this study we give evidence that domperidone encapsulated into amphiphilic p(HPMA)-co-p(laurylmethacrylate) (LMA) copolymer aggregates is able to cross the blood-brain barrier, since it affected motor behaviour in animals, which is a sensitive measure for CNS actions. Carefully designed copolymers based on the clinically approved p(HPMA) were selected and synthesized by a combination of controlled radical polymerization and post-polymerization modification. The hydrodynamic radii (R(h) ) of amphiphilic p(HPMA)-co-p(LMA) alone and loaded with domperidone were determined by fluorescence correlation spectroscopy.Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.