HPMA based amphiphilic copolymers mediate central nervous effects of domperidone

Macromol Rapid Commun. 2011 May 18;32(9-10):712-7. doi: 10.1002/marc.201000810. Epub 2011 Apr 5.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood-Brain Barrier / drug effects
  • Central Nervous System / drug effects*
  • Domperidone / chemistry
  • Domperidone / pharmacology*
  • Dopamine Antagonists / chemistry
  • Dopamine Antagonists / pharmacology
  • Drug Carriers / chemistry*
  • Drug Delivery Systems / instrumentation*
  • Male
  • Methacrylates / chemistry*
  • Mice
  • Polymers / chemical synthesis
  • Polymers / chemistry*

Substances

  • Dopamine Antagonists
  • Drug Carriers
  • Methacrylates
  • Polymers
  • Domperidone
  • hydroxypropyl methacrylate