Preparation, in vitro and in vivo evaluation of polymeric nanoparticles bas hyaluronic acid-poly(but-资料下载-美国布鲁克海文仪器公司

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Herein, we describe the preparation of a targeted cellular delivery system for morin hydrate (MH),

-molecular-weight hyaluronic acid-poly(butyl cyanoacrylate) (HA-PBCA) block copolymer. In ord

the therapeutic effect of MH, D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) was

HA-PBCA during the preparation process. The MH-loaded HA-PBCA “plain” nanoparticle (MH-P

PBCA/TPGS “mixed” nanoparticles (MH-MNs) were concomitantly characterized in terms of load

particle size, zeta potential, critical aggregation concentration, and morphology. The obtained MHMNs

exhibited a spherical morphology with a negative zeta potential and a particle size less than 2

favorable for drug targeting. Remarkably, the addition of TPGS resulted in about 1.6-fold increase

loading. The in vitro cell viability experiment revealed that MH-MNs enhanced the cytotoxicity of

cells compared with MH solution and MH-PNs. Furthermore, blank MNs containing TPGS exhibit

cytotoxic effects against cancer cells without diminishing the viability of normal cells. In addition,

uptake study indicated that MNs resulted in 2.28-fold higher cellular uptake than that of PNs, in A5

CD44 receptor competitive inhibition and the internalization pathway studies suggested that the int

mechanism of the nanoparticles was mediated mainly by the CD44 receptors through a clathrin-dep

endocytic pathway. More importantly, MH-MNs exhibited a higher in vivo antitumor potency and

tumor cell apoptosis than did MH-PNs, following intravenous administration to S180 tumor-bearin

Overall, the results imply that the developed nanoparticles are promising vehicles for the targeted d

lipophilic anticancer drugs.

Keywords: anti-tumor effect, hyaluronic acid, TPGS, morin hydrate, nanoparticles