Tumor specificity and therapeutic efficacy of photosensitizer-encapsulated glycol chitosan-based nanoparticles in tumor-bearing mice

So Jin Lee, Kyeongsoon Park, Yu Kyoung Oh, Seung Hae Kwon, Songwook Her, In San Kim, Kuiwon Choi, Sung Jun Lee, Hoyoung Kim, Se Geun Lee, Kwangmeyung Kim, Ick Chan Kwon

Research output: Contribution to journalArticlepeer-review

164 Scopus citations


We reported the development of new nanoscale drug carriers, chitosan-based nanoparticles (CNPs) that can be used for photodynamic therapy. These carriers could encapsulate a photosensitizer, protophorphyrin IX (PpIX), and deliver it to tumor tissue. We already reported that CNPs presented the enhanced tumor target specificity in cancer therapy and imbibed various water insoluble anticancer agents into the hydrophobic multicores of nanoscale particles. In this study, we prepared photosensitizer-encapsulated CNPs by self-assembling amphiphilic glycol chitosan-5β-cholanic acid conjugates in an aqueous environment and then encapsulating the water-insoluble photosensitizer (PpIX), with high drug-loading efficiency (>90%) by using a dialysis method. Freshly prepared PpIX-encapsulated CNPs (PpIX-CNPs) had an average diameter of 290 nm and were stable in aqueous solutions for 1 month. As nanoscale drug carriers, PpIX-CNPs exhibited a sustained release profile in vitro and were non-toxic to tumor cells in the dark. In a cell culture system, we observed rapid cellular uptake of the PpIX-CNPs and the released PpIX from CNPs became highly phototoxic upon visible irradiation. In SCC7 tumor-bearing mice, PpIX-CNPs exhibited enhanced tumor specificity and increased therapeutic efficacy compared to free PpIX. Taken together, our results indicate that PpIX-CNPs have potential as an effective drug delivery system for clinical photodynamic therapy.

Original languageEnglish
Pages (from-to)2929-2939
Number of pages11
Issue number15
StatePublished - May 2009

Bibliographical note

Funding Information:
This research was financially supported by the Real-Time Molecular Imaging Project, F104AA010003-06A0101-00310 of MEST, by the Seoul R&D program, by the Korea Government (MOEHRD, Basic Research Promotion Fund) (KRF-2007-412-J00304) and by a grant of the Advanced Medical Technology Cluster for Diagnosis and Prediction at Kyungpook National University, awarded by MOCIE.


  • Chitosan-based nanoparticles
  • Drug delivery system
  • Photodynamic therapy
  • Photosensitizer
  • Tumor target specificity


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