Transferrin-conjugated polyphosphoester hybrid micelle loading paclitaxel for brain-targeting delivery: Synthesis, preparation and in vivo evaluation

Pengcheng Zhang, Luojuan Hu, Qi Yin, Zhiwen Zhang, Linyin Feng, Yaping Li

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122 Citations (Scopus)


The successful treatment of central nervous system (CNS) disorders is hampered by inefficient drug delivery across the blood-brain barrier (BBB). Transferrin (Tf) could facilitate the transcytosis of coupled nanocarriers through Tf receptor (TfR) mediated pathway. In this study, Tf-modified paclitaxel-loaded polyphosphoester hybrid micells (TPM) was prepared and evaluated for its in vitro and in vivo brain-targeting efficiency. The polyphosphoester hybrid micelle formed a core-shell structure in aqueous solution, and demonstrated high drug entrapping efficiency (89.9 ± 3.4%). In addition, the micelle showed negligible hemolysis even at 2.0 mg/mL. The TPM was 87.85 ± 2.32 nm with ζ potentials - 12.33 ± 1.46 mV, and PTX showed sustained release from TPM. TPM demonstrated enhanced cellular uptake and brain accumulation, which were 2 and 1.8-fold of PM, respectively. TPM exhibited strongest anti-glioma activity, and the mean survival time of mice bearing intracranial U-87 MG glioma treated with TPM (39.5 days) was significantly longer than those treated with Taxol® (33.6 days). These results indicated that Tf conjugated micelle could be a promising carrier for brain-targeting drug delivery.

Original languageEnglish
Pages (from-to)429-434
Number of pages6
JournalJournal of Controlled Release
Issue number3
Publication statusPublished - 10 May 2012
Externally publishedYes


  • Blood-brain barrier (BBB)
  • Glioma
  • Micelle
  • Polyphosphoester
  • Transferrin

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