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• W2787117586 startingPage "1302" @default.
• W2787117586 abstract "It was reported that the shape of nanocarriers played an important role in achieving a better therapeutic effect. To optimize the morphology and enhance the antitumor efficacy, in this study based on the amphiphilic PAMAM- b-OEG codendrimer (POD), docetaxel-loaded spherical and flake-like nanoparticles (DTX nanospheres and nanosheets) were prepared via an antisolvent precipitation method with similar particle size, surface charge, stability, and release profiles. The feed weight ratio of DTX/POD and the branched structure of OEG dendron were suggested to influence the shapes of the self-assembled nanostructures. As expected, DTX nanospheres and nanosheets exhibited strong shape-dependent cellular internalization efficiency and antitumor activity. The clathrin-mediated endocytosis and macropincytosis-dependent endocytosis were proven to be the main uptake mechanism for DTX nanospheres, while it was clathrin-mediated endocytosis for DTX nanosheets. More importantly, DTX nanosheets presented obviously superior antitumor efficacy over nanospheres, the tumor inhibition rate was increased 2-fold in vitro and 1.3-fold in vivo. An approximately 2-fold increase in pharmacokinetic parameter (AUC, MRT, and T1/2) and tumor accumulation were observed in the DTX nanosheets group. These results suggested that the particle shape played a key role in influencing cellular uptake behavior, pharmacokinetics, biodistribution, and antitumor activity; the shape of drug-loaded nanoparticles should be considered in the design of a new generation of nanoscale drug delivery systems for better therapeutic efficacy of anticancer drug." @default.
• W2787117586 created "2018-02-23" @default.
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• W2787117586 date "2018-02-09" @default.
• W2787117586 modified "2023-10-18" @default.
• W2787117586 title "Shape of Nanoparticles as a Design Parameter to Improve Docetaxel Antitumor Efficacy" @default.
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• W2787117586 doi "https://doi.org/10.1021/acs.bioconjchem.8b00059" @default.
• W2787117586 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29426226" @default.
• W2787117586 hasPublicationYear "2018" @default.
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