4.7 Article

Hyaluronic acid-grafted polyamidoamine dendrimers enable long circulation and active tumor targeting simultaneously

期刊

CARBOHYDRATE POLYMERS
卷 126, 期 -, 页码 231-239

出版社

ELSEVIER SCI LTD
DOI: 10.1016/j.carbpol.2015.03.019

关键词

Polyamidoamine dendrimers; Hyaluronic acid; Topotecan hydrochloride; Tumor targeting; Tumor therapy; Nanoparticles

资金

  1. Fundamental Research Funds for the Central Universities [2015ZD007, 2015PT052]
  2. National Natural Science Foundation of China [81402859]
  3. Natural Science Foundation of Jiangsu Province [BK20130663]

向作者/读者索取更多资源

Herein, we developed dualfunctional hyaluronic acid (HA)-grafted polyamidoamine (PAMAM) dendrimers for simultaneous systemic long circulation and active tumor targeting and delivery of topotecan hydrochloride (TPT). The possibility of these modified dendrimers as nanocarriers for promoting tissue distribution and antitumor efficiency, as well as a drug release profile, cytotoxicity and cellular uptake, was investigated, The fine targeting efficiency of HA-PAMAM/TPT was confirmed by the CD44 receptor-mediated high cellular uptake efficiency and low cytotoxicity in HCT-116 cells, and the in vivo higher tumor distribution percentage than in other tissues in mice bearing an S-180 tumor. Pharmacokinetic studies showed that the t(1/2) and MRT of TPT were significantly extended after intravenous administration of HA-PAMAM/TPT in normal rats. Moreover, TPT-loaded nanovehicles demonstrated higher antitumor activity compared with free drug and PAMAM/TPT. Overall, HA-PAMAM may be an alternative vector for the effective targeted delivery of and tumor therapy with antitumor drugs. (C) 2015 Elsevier Ltd. All rights reserved.

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