Evaluation of polyanion-coated biodegradable polymeric micelles as drug delivery vehicles

Yuichi Ohya, Shinya Takeda, Yosuke Shibata, Tatsuro Ouchi, Arihiro Kano, Tomoki Iwata, Shinichi Mochizuki, Yuki Taniwaki, Atsushi Maruyama

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32 Citations (Scopus)

Abstract

Polymeric micelles, as drug delivery vehicles, must achieve specific targeting and high stability in the body for efficient drug delivery. We recently reported the preparation of polyanion-coated biodegradable polymeric micelles by coating positively charged polymeric micelles consisting of poly(l-lysine)-block-poly(l-lactide) (PLys-b-PLLA) AB diblock copolymers with anionic hyaluronic acid (HA) by polyion complex (PIC) formation. The obtained HA-coated micelles showed significantly higher stability in aqueous solution. In this study, to evaluate the HA-coated polymeric micelles as a drug carrier, model drug release from the micelles and cytotoxicity of the micelles were investigated. The HA-coated micelles showed sustained release of model drugs and low cytotoxicity. It is known that there are receptors for HA on liver sinusoidal endothelial cells (LSEC). Specific interactions of HA-coated micelles with LSECs and Kupffer cells were investigated and compared with polymeric micelles coated with other polyanionic polysaccharides, i.e., heparin (Hep) and carboxymethyl-dextran (CMDex). Although Hep-coated micelles and CMDex-coated micelles were incorporated into both Kupffer cells and LSECs, HA-coated micelles were taken up only into LSECs. These results suggest HA-coated micelles have potential utility as drug delivery vehicles exhibiting specific accumulation into LSECs.

Original languageEnglish
Pages (from-to)104-110
Number of pages7
JournalJournal of Controlled Release
Volume155
Issue number1
DOIs
Publication statusPublished - Oct 10 2011

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All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

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