Biocompatibility, cellular uptake and biodistribution of the polymeric amphiphilic nanoparticles as oral drug carriers

Ya Liu, Ming Kong, Chao Feng, Kui Kun Yang, Yang Li, Jing Su, Xiao Jie Cheng, Hyun Jin Park, Xi Guang Chen

Research output: Contribution to journalArticlepeer-review

47 Citations (Scopus)


Oleoyl-carboxymethyl-chitosan (OCMCS) was synthesized and were soluble at neutral pH. The critical micelle concentration (CMC) of OCMCS in deionized water was 0.021. mg/ml. OCMCS nanoparticles were successfully prepared via self-assembly with mean diameter of 215.34. nm, zeta potential of 19.26. mV and an almost spherical shape as determined by electron microscopy. The OCMCS nanoparticles showed low erythrocyte membrane-damaging effect. The MTT survival assay indicated no significant cytotoxicity to Caco-2 cells and MEFs cells. The uptake of FITC labeled OCMCS nanoparticles by Caco-2 cells was confirmed via confocal laser scanning microscope (CLSM). In vivo toxicity assays were performed via histopathological evaluation, and no specific anatomical pathological changes or tissue damage was observed in the tissues of carps. The extent of tissue distribution and retention following oral administration of FITC-OCMCS nanoparticles was analyzed for 3 days. After 3 days, the nanoparticles remained detectable in the muscle, heart, kidney, liver, intestine, and spleen. The results showed that 34.32% of the particles were localized in the liver, 18.79% in the kidney, and 17.36% in the heart. The lowest percentage was observed in the muscle. These results implied that OCMCS nanoparticles had great potential to be applied as safe carriers for the oral administration of protein drugs.

Original languageEnglish
Pages (from-to)345-353
Number of pages9
JournalColloids and Surfaces B: Biointerfaces
Publication statusPublished - 2013 Mar 1

Bibliographical note

Funding Information:
This work was supported by grants from the National Natural Science Foundation of China (NSFC , 81071274 ) and Key Project of Science and Technology, Department of Zhejiang of China ( 2011GSF12124 ).


  • Biocompatibility
  • Biodistribution
  • Cellular uptake
  • Nanoparticles

ASJC Scopus subject areas

  • Biotechnology
  • Surfaces and Interfaces
  • Physical and Theoretical Chemistry
  • Colloid and Surface Chemistry


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