Comparative study of photosensitizer loaded and conjugated glycol chitosan nanoparticles for cancer therapy

So Jin Lee, Heebeom Koo, Hayoung Jeong, Myung Sook Huh, Yongseok Choi, Seo Young Jeong, Youngro Byun, Kuiwon Choi, Kwangmeyung Kim, Ick Chan Kwon

Research output: Contribution to journalArticlepeer-review

190 Citations (Scopus)


This study reports that tumor-targeting glycol chitosan nanoparticles with physically loaded and chemically conjugated photosensitizers can be used in photodynamic therapy (PDT). First, the hydrophobic photosensitizer, chlorin e6 (Ce6), was physically loaded onto the hydrophobically-modified glycol chitosan nanoparticles (HGC), which were prepared by self-assembling amphiphilic glycol chitosan-5β-cholanic acid conjugates under aqueous conditions. Second, the Ce6s were chemically conjugated to the glycol chitosan polymers, resulting in amphiphilic glycol chitosan-Ce6 conjugates that formed self-assembled nanoparticles in aqueous condition. Both Ce6-loaded glycol chitosan nanoparticles (HGC-Ce6) and Ce6-conjugated chitosan nanoparticles (GC-Ce6) had similar average diameters of 300 to 350 nm, a similar in vitro singlet oxygen generation efficacy under buffer conditions, and a rapid cellular uptake profile in the cell culture system. However, compared to GC-Ce6, HGC-Ce6 showed a burst of drug release in vitro, whereby 65% of physically loaded drugs were rapidly released from the particles within 6.5 h in the buffer condition. When injected through the tail vein into tumor bearing mice, HGC-Ce6 did not accumulate efficiently in tumor tissue, reflecting the burst in the release of the physically loaded drug, while GC-Ce6 showed a prolonged circulation profile and a more efficient tumor accumulation, which resulted in high therapeutic efficacy. These comparative studies with drug-loaded and drug-conjugated nanoparticles showed that the photosensitizer-conjugated glycol chitosan nanoparticles with excellent tumor targeting properties have potential for PDT in cancer treatment.

Original languageEnglish
Pages (from-to)21-29
Number of pages9
JournalJournal of Controlled Release
Issue number1
Publication statusPublished - 2011 May 30


  • Drug-conjugated nanoparticle
  • Drug-loaded nanoparticle
  • Glycol chitosan
  • Photodynamic therapy
  • Photosensitizer

ASJC Scopus subject areas

  • Pharmaceutical Science


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