title: HPMA based amphiphilic copolymers mediate central nervous effects of domperidone.
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.
authors.affiliation: Institute of Organic Chemistry, Johannes Gutenberg University Mainz, Duesbergweg 10-14, Mainz, Germany.
authors.forename: Mirjam
authors.initials: M
authors.lastname: Hemmelmann
authors.forename: Christiane
authors.initials: C
authors.lastname: Knoth
authors.forename: Ulrich
authors.initials: U
authors.lastname: Schmitt
authors.forename: Mareli
authors.initials: M
authors.lastname: Allmeroth
authors.forename: Dorothea
authors.initials: D
authors.lastname: Moderegger
authors.forename: Matthias
authors.initials: M
authors.lastname: Barz
authors.forename: Kaloian
authors.initials: K
authors.lastname: Koynov
authors.forename: Christoph
authors.initials: C
authors.lastname: Hiemke
authors.forename: Frank
authors.initials: F
authors.lastname: Rösch
authors.forename: Rudolf
authors.initials: R
authors.lastname: Zentel
mesh_terms: D000818:Animals; D001812:Blood-Brain Barrier / Q000187:drug effects; D002490:Central Nervous System / Q000187:drug effects*; D004294:Domperidone / Q000737:chemistry / Q000494:pharmacology*; D018492:Dopamine Antagonists / Q000737:chemistry / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000295:instrumentation*; D008297:Male; D008689:Methacrylates / Q000737:chemistry*; D051379:Mice; D011108:Polymers / Q000138:chemical synthesis / Q000737:chemistry*
chemical_list: D018492:Dopamine Antagonists; D004337:Drug Carriers; D008689:Methacrylates; D011108:Polymers; D004294:Domperidone; C032802:hydroxypropyl methacrylate