Nanoscopic micelle delivery improves the photophysical properties and efficacy of photodynamic therapy of protoporphyrin IX

Huiying Ding, Baran D. Sumer, Chase W. Kessinger, Ying Dong, Gang Huang, David A. Boothman, Jinming Gao

Research output: Contribution to journalArticlepeer-review

102 Scopus citations

Abstract

Nanodelivery systems have shown considerable promise in increasing the solubility and delivery efficiency of hydrophobic photosensitizers for photodynamic therapy (PDT) applications. In this study, we report the preparation and characterization of polymeric micelles that incorporate protoporphyrin IX (PpIX), a potent photosensitizer, using non-covalent encapsulation and covalent conjugation methods. Depending on the incorporation method and PpIX loading percentage, PpIX existed as a monomer, dimer or aggregate in the micelle core. The PpIX state directly affected the fluorescence intensity and 1O2 generation efficiency of the resulting micelles in aqueous solution. Micelles with lower PpIX loading density (e.g. 0.2%) showed brighter fluorescence and higher 1O2 yield than those with higher PpIX loading density (e.g. 4%) in solution. However, PDT efficacy in H2009 lung cancer cells showed an opposite trend. In particular, 4% PpIX-conjugated micelles demonstrated the largest PDT therapeutic window, as indicated by the highest phototoxicity and relatively low dark toxicity. Results from this study contribute to the fundamental understanding of nanoscopic structure-property relationships of micelle-delivered PpIX and establish a viable micelle formulation (i.e. 4% PpIX-conjugated micelles) for in vivo evaluation of antitumor efficacy.

Original languageEnglish (US)
Pages (from-to)271-277
Number of pages7
JournalJournal of Controlled Release
Volume151
Issue number3
DOIs
StatePublished - May 10 2011

Keywords

  • Nanoparticle delivery
  • Photodynamic therapy
  • Photosensitizer
  • Polymeric micelles
  • Protoporphyrin IX
  • Singlet oxygen

ASJC Scopus subject areas

  • Pharmaceutical Science

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