A novel lactoferrin-modified β-cyclodextrin nanocarrier for brain-targeting drug delivery

Yajing Ye, Yi Sun, Hongli Zhao, Minbo Lan, Feng Gao, Chao Song, Kaiyan Lou, Hao Li, Wei Wang

Research output: Contribution to journalArticlepeer-review

49 Scopus citations


The blood-brain barrier (BBB) restricts the transfer and delivery of most drug substances to brain. In this study, a novel nano-drug delivery system for brain-targeting was developed and investigated in vitro and in vivo. Lactoferrin (Lf) was selected as a brain-targeting ligand and conjugated to β-cyclodextrin (β-CD) via the heterobifunctional polyethyleneglycol (PEG) linker NHS-PEG-MAL, yielding Lf conjugated β-cyclodextrin (Lf-CD). UV-vis, FTIR, NMR and transmission electron microscopy (TEM) techniques clearly demonstrated the successful synthesis of Lf-CD nanoparticles with the average diameter of 92.9 ± 16.5 nm. Using near-infrared fluorescent dye IR-775 chloride (IR) as a model compound of poorly water-soluble drugs, IR-loaded Lf-CD nanoparticles (Lf-CD/IR) were successfully prepared with a high entrapment efficiency of 98.1 ± 4.8%. Biodistribution and pharmacokinetics of Lf-CD/IR were evaluated in KM mice after intravenous administration. The results of tissue distribution studies revealed that Lf-CD/IR treatment showed greatly improved BBB transport efficiency. In addition, AUC0-2 h of IR in brain after Lf-CD/IR treatment was seven fold higher compared with that of IR treatment without Lf-CD nano-carriers, demonstrating that the introduction of Lf-CD drug-delivery system positively resulted in a higher AUC located in brain tissue. These results provide evidence that Lf-CD nanoparticles could be exploited as a potential brain-targeting drug delivery system for hydrophobic drugs and diagnostic reagents which normally fail to pass through the BBB.

Original languageEnglish (US)
Pages (from-to)110-117
Number of pages8
JournalInternational Journal of Pharmaceutics
Issue number1
StatePublished - 2013
Externally publishedYes


  • Brain-targeting
  • Lactoferrin
  • Nano-drug delivery system
  • Transferrin
  • beta;-cyclodextrin derivatives

ASJC Scopus subject areas

  • Pharmaceutical Science


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