Effect of particle size on their accumulation in an inflammatory lesion in a dextran sulfate sodium (DSS)-induced colitis model

Ayaka Watanabe, Hiroki Tanaka, Yu Sakurai, Kota Tange, Yuta Nakai, Tatsuya Ohkawara, Hiroshi Takeda, Hideyoshi Harashima, Hidetaka Akita

Research output: Contribution to journalArticlepeer-review

34 Citations (Scopus)


Taking advantage of the enhanced permeation and retention (EPR) effect is a promising approach for delivering macromolecules or nanoparticles to tumors. Recent studies revealed that this strategy is also applicable for targeting other pathological lesions (i.e. inflammatory disease). In the present study, we report the optimal size of a nanoparticle for allowing the higher accumulation of a particle in an inflammatory lesion using a dextran sulfate sodium (DSS)-induced colitis model. As a nanoparticle platform, we utilized a SS-cleavable and pH-activated lipid-like material (ssPalm), that can be used to produce particles in a variety of sizes ranging from 50 nm to 180 nm while using the same lipid composition. In healthy mice, particle accumulation remained low regardless of size. In contrast, the accumulation in inflammatory colon tissue was enhanced depending on the progress of the inflammation. In this situation, the apparent uptake clearance accumulation of a mid-sized particle (113 nm on average) was higher than that for smaller and larger (54 nm and 183 nm in average, respectively) ones. Therefore, controlling particle size is an important parameter for the extensive targeting of inflammatory lesion.

Original languageEnglish
Pages (from-to)118-122
Number of pages5
JournalInternational Journal of Pharmaceutics
Issue number1-2
Publication statusPublished - 2016 Jul 25
Externally publishedYes


  • Accumulation
  • Colitis
  • Inflammation
  • Nanoparticles
  • ssPalm

ASJC Scopus subject areas

  • Pharmaceutical Science


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