Hydrophobically modified glycol chitosan nanoparticles as carriers for paclitaxel

Jong Ho Kim, Yoo Shin Kim, Sungwon Kim, Jae Hyung Park, Kwangmeyung Kim, Kuiwon Choi, Hesson Chung, Seo Young Jeong, Rang Woon Park, In San Kim, Ick Chan Kwon

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275 Citations (Scopus)

Abstract

Self-assembled nanoparticles based on hydrophobically modified glycol chitosan (HGC) were prepared as a carrier for paclitaxel. HGC conjugates were prepared by chemically linking 5β-cholanic acid to glycol chitosan chains using 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide chemistry. In phosphate-buffered saline (PBS; pH 7.4), the synthesized HGC conjugates formed nano-sized particles with a diameter of 200 nm and exhibited high thermodynamic stability as reflected by their low critical aggregation concentration (0.03 mg/ml). Paclitaxel was efficiently loaded into HGC nanoparticles up to 10 wt.% using a dialysis method. The paclitaxel-loaded HGC (PTX-HGC) nanoparticles were 400 nm in diameter and were stable in PBS for 10 days. These PTX-HGC nanoparticles also showed sustained release of the incorporated of paclitaxel (80% of the loaded dose was released in 8 days at 37°C in PBS). Owing to sustained release, the PTX-HGC nanoparticles were less cytotoxic to B16F10 melanoma cells than free paclitaxel formulated in Cremophor EL. Injection of PTX-HGC nanoparticles into the tail vein of tumor-bearing mice prevented increases in tumor volume for 8 days. Finally, PTX was less toxic to the tumor-bearing mice when formulated in HGC nanoparticles than when formulated with Cremophor EL.

Original languageEnglish
Pages (from-to)228-234
Number of pages7
JournalJournal of Controlled Release
Volume111
Issue number1-2
DOIs
Publication statusPublished - 2006 Mar 10

Keywords

  • Hydrophobically modified glycol chitosan
  • In vivo anti-tumor effect
  • Nanoparticles
  • Paclitaxel

ASJC Scopus subject areas

  • Pharmaceutical Science

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  • Cite this

    Kim, J. H., Kim, Y. S., Kim, S., Park, J. H., Kim, K., Choi, K., Chung, H., Jeong, S. Y., Park, R. W., Kim, I. S., & Kwon, I. C. (2006). Hydrophobically modified glycol chitosan nanoparticles as carriers for paclitaxel. Journal of Controlled Release, 111(1-2), 228-234. https://doi.org/10.1016/j.jconrel.2005.12.013