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

研究成果: ジャーナルへの寄稿学術誌査読

43 被引用数 (Scopus)


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.

ジャーナルJournal of Controlled Release
出版ステータス出版済み - 10月 10 2011

All Science Journal Classification (ASJC) codes

  • 薬科学


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