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High-loading nanosized micelles of copoly(styrene-maleic acid)-zinc protoporphyrin for targeted delivery of a potent heme oxygenase inhibitor.

Abstract
Amphiphilic styrene-maleic acid (SMA) copolymer efficiently formed micelles with a potent heme oxygenase inhibitor-zinc protoporphyrin (ZnPP). The micelles were constructed by subtle pH adjustments to form non-covalent interaction between the hydrophobic ZnPP and amphiphilic SMA. The micelles (SMA-ZnPP) thus formed were nanoparticles with narrow size distribution in water (mean diameter 176.5nm), having tunable loading (from 15% to 60% w/w of ZnPP) with remarkable aqueous solubility. SMA-ZnPP had an average molecular size of 144kDa as determined by size-exclusion chromatography (SEC), this size is a marked increase from the molecular weight of free ZnPP (626.03Da), suggesting the formation of micellar structure. The micelles showed a constant ZnPP release rate of about 0.5%/day in vitro at neutral pH. SMA-ZnPP micelles inhibited splenic microsomal HO-1 activity, in a competitive and dose-dependent manner, with an apparent inhibitory constant (K(i)) of 0.12mum, comparable to free ZnPP and also exhibited marked cytotoxic effect on KYSE-510 human esophageal cancer cells. The unique features of SMA-ZnPP micelles are that they are nanoparticles in aqueous solution having high water solubility and loading, yet macromolecular in nature, which can be beneficial in targeted release of a potent HO-1 inhibitor.
AuthorsArun K Iyer, Khaled Greish, Jun Fang, Ryoichi Murakami, Hiroshi Maeda
JournalBiomaterials (Biomaterials) Vol. 28 Issue 10 Pg. 1871-81 (Apr 2007) ISSN: 0142-9612 [Print] Netherlands
PMID17208294 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Biocompatible Materials
  • Maleates
  • Metalloporphyrins
  • Micelles
  • Polystyrenes
  • Protoporphyrins
  • copoly(styrene-maleic acid)-zinc protoporphyrin
  • zinc protoporphyrin
  • Heme Oxygenase (Decyclizing)
Topics
  • Biocompatible Materials (chemistry)
  • Diffusion
  • Drug Delivery Systems (methods)
  • Drug Stability
  • Heme Oxygenase (Decyclizing) (antagonists & inhibitors)
  • Maleates (chemistry)
  • Materials Testing
  • Metalloporphyrins (chemistry)
  • Micelles
  • Nanostructures (chemistry, ultrastructure)
  • Particle Size
  • Polystyrenes (chemistry)
  • Protoporphyrins (administration & dosage, chemistry)

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