Hydrophobically modified glycol chitosan nanoparticles-encapsulated camptothecin enhance the drug stability and tumor targeting in cancer therapy

Kyung Hyun Min, Kyeongsoon Park, Yoo Shin Kim, Sang Mun Bae, Seulki Lee, Hyung Gon Jo, Rang Woon Park, In San Kim, Seo Young Jeong, Kwangmeyung Kim, Ick Chan Kwon

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To prepare a water-insoluble camptothecin (CPT) delivery carrier, hydrophobically modified glycol chitosan (HGC) nanoparticles were constructed by chemical conjugation of hydrophobic 5β-cholanic acid moieties to the hydrophilic glycol chitosan backbone. Insoluble anticancer drug, CPT, was easily encapsulated into HGC nanoparticles by a dialysis method and the drug loading efficiency was above 80%. CPT-encapsulated HGC (CPT-HGC) nanoparticles formed nano-sized self-aggregates in aqueous media (280-330 nm in diameter) and showed sustained release of CPT for 1 week. Also, HGC nanoparticles effectively protected the active lactone ring of CPT from the hydrolysis under physiological condition, due to the encapsulation of CPT into the hydrophobic cores in the HGC nanoparticles. The CPT-HGC nanoparticles exhibited significant antitumor effects and high tumor targeting ability towards MDA-MB231 human breast cancer xenografts subcutaneously implanted in nude mice. Tumor growth was significantly inhibited after i.v. injection of CPT-HGC nanoparticles at doses of 10 mg/kg and 30 mg/kg, compared to free CPT at dose of 30 mg/kg. The significant antitumor efficacy of CPT-HGC nanoparticles was attributed to the ability of the nanoparticles to show both prolonged blood circulation and high accumulation in tumors, as confirmed by near infrared (NIR) fluorescence imaging systems. Thus, the delivery of CPT to tumor tissues at a high concentration, with the assistance of HGC nanoparticles, exerted a potent therapeutic effect. These results reveal the promising potential of HGC nanoparticles-encapsulated CPT as a stable and effective drug delivery system in cancer therapy.

Original languageEnglish
Pages (from-to)208-218
Number of pages11
JournalJournal of Controlled Release
Issue number3
StatePublished - 8 May 2008

Bibliographical note

Funding Information:
This research was financially supported by the Ministry of Science and Technology (F104AA010003-06A0101-00310) in Korea, by BK21 BNT Scientist Renovating for the Drug Development Coping with Aged Society, and by Seoul R&BD Program.


  • Anticancer drug delivery system
  • Breast cancer
  • Camptothecin (CPT)
  • Cancer therapy
  • Hydrophobically modified glycol chitosan nanoparticles (HGC)


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