Synthesis of Bile-acid-carrying Polymer and Its Application in Surface Modification of Nanoparticles for Hepatic Cell Targeting
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R632.3;R944.9

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    Abstract:

    Bile acid transporter, which is aboundent on the hepatic cell surface, provides a promising way accessing the hepatic cell targeted drug delivery. In the present study, poly-[3 alpha-(4-vinylbenzonate)-7 alpha,12 alpha-dihydroxy-5 beta-cholan-24-oic acid] (PVBCA), a amphiphilic polymer with bile acid structure in the side-chain, was designed and synthesized. PVBCA coated PLGA nanoparticles with the diameter of 350nm were prepared by emulsion-solvent evaporation method and PVBCA assembled on the nanoparticle surface due to its amphiphilicity. The specific interactions between PVBCA and hepatic cells, as well as the uptake of the PVBCA coated PLGA nanoparticles were evaluated by SMMC-7721 cells in vitro, with fluorescent probe coumarin 6 employed as the model drug. The results showed the cells absorbed on the PVBCA film were more than the twice of those absorbed on the polystyrene surface of culture dash. In comparison with the delivery by unmodified nanoparticles, the intracellular concentration of coumarin 6 was increased by more than 8 times with the vehicle of PVBCA coated nanoparticle. In conclusion, PVBCA, as the nanopartice-coating polymer, exhibited significant potential in liver-targeted drug delivery.

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History
  • Received:August 02,2011
  • Revised:September 06,2011
  • Adopted:September 08,2011
  • Online: October 25,2011
  • Published:
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