A 5-fluorouracil-loaded pH-responsive dendrimer nanocarrier for tumor targeting

Yiguang Jin, Xia Ren, Wei Wang, Lijing Ke, Erjuan Ning, Lina Du, Jeremy Bradshaw

Research output: Contribution to journalArticlepeer-review

Abstract / Description of output

A novel long-circulating and pH-responsive dendrimer nanocarrier was prepared for delivering 5-fluorouracil (5-FU) to tumors through the targeting of nanoparticles to the low pH environment of tumors. The nanocarrier, poly(2-(N,N-diethylamino)ethyl methacrylate) with methoxy-poly(ethylene glycol)-poly(amidoamine) (PPD), had a core-shell structure with 4.0 G poly(amidoamine) (PAMAM) as the core and parallel poly(2-(N,N-diethylamino)ethyl methacrylate) (PDEA) chains and methoxy-poly(ethylene glycol) (mPEG) chains as the shell. The PDEA chain was pH-responsive, and the PEG chains led to long circulation in blood vessels to achieve tumor targeting. The sizes, drug encapsulation and release of PPD nanocarriers showed high pH-dependency due to the PDEA chains, as they were hydrophilic at pH 6.5 and hydrophobic at pH 7.4. The encapsulation efficiency of 5-FU in PPD nanocarriers was as high as 92.5% through the pH transition. The release of 5-FU from PPD nanocarriers was much faster at pH 6.5 than at pH 7.4. The 5-FU-loaded nanocarrier had a long half-life after intravenous administration in mice and showed high tumor targeting. This nanocarrier composite also showed enhanced anticancer effects. PPD is a promising nanocarrier of anticancer drugs with high encapsulation, tumor targeting and pH-responsive release in tumors.
Original languageEnglish
Pages (from-to)378-384
Number of pages7
JournalInternational Journal of Pharmaceutics
Issue number2
Publication statusPublished - Nov 2011

Keywords / Materials (for Non-textual outputs)

  • 5-Fluorouracil
  • Nanocarriers
  • pH-responsive
  • Poly(amidoamine)
  • Tumor targeting


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