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Issue 2, 2014
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pH-sensitive pullulan-based nanoparticles for intracellular drug delivery

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This study reports the design of a novel pH-sensitive nanoparticle carrier based on pullulan for realizing intracellular drug delivery. A series of pullulan derivatives (UCPA) were synthesized by conjugation of both urocanic acid (a pH-sensitive grafted moiety) and cholesterol succinate (a hydrophobically modified moiety) to pullulan. UCPAs exhibited amphiphilic and pH-sensitive properties, and their responding pH value was around 6.5. UCPA nanoparticles prepared by the precipitation method had roughly spherical shapes, and sizes ranging from 150 to 300 nm. Doxorubicin (DOX), as a model antitumor drug, was physically loaded into the UCPA nanoparticles and its in vitro release at different pH values was studied using a dialysis method. UCPA-1 nanoparticles, with the degree of substitution (DS) of urocanyl and cholesterol moieties of 6.8% and 3.5%, respectively, exhibited relatively high drug-loading capability and strong in vitro pH-induced drug release. The results of MTT assays, flow cytometric analyses and confocal microscopy observations confirmed that the UCPA-1 nanoparticles can realize the intracellular delivery of DOX after internalization and enhanced cytotoxicity of DOX against MCF-7 cells.

Graphical abstract: pH-sensitive pullulan-based nanoparticles for intracellular drug delivery

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The article was received on 21 Jun 2013, accepted on 27 Aug 2013 and first published on 29 Aug 2013

Article type: Paper
DOI: 10.1039/C3PY00817G
Citation: Polym. Chem., 2014,5, 423-432
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    pH-sensitive pullulan-based nanoparticles for intracellular drug delivery

    Y. Wang, Y. Liu, Y. Liu, Y. Wang, J. Wu, R. Li, J. Yang and N. Zhang, Polym. Chem., 2014, 5, 423
    DOI: 10.1039/C3PY00817G

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