PEGylated Poly(amidoamine) dendrimer-based dual-targeting carrier for treating brain tumors

被引：261

作者：

He, Hai ^{[1
,2
]}

Li, Yan ^{[1
,2
]}

Jia, Xin-Ru ^{[1
,2
]}

Du, Ju ^{[3
,4
]}

Ying, Xue ^{[3
,4
]}

Lu, Wan-Liang ^{[3
,4
]}

Lou, Jin-Ning ^{[5
]}

Wei, Yan ^{[6
]}

机构：

[1] Peking Univ, Coll Chem & Mol Engn, Minist Educ, Beijing Natl Lab Mol Sci, Beijing 100871, Peoples R China

[2] Peking Univ, Coll Chem & Mol Engn, Minist Educ, Key Lab Polymer Chem & Phys, Beijing 100871, Peoples R China

[3] Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100871, Peoples R China

[4] Peking Univ, Sch Pharmaceut Sci, Beijing 100871, Peoples R China

[5] Minist Hlth, China Japan Friendship Hosp, Inst Clin Med Sci, Beijing, Peoples R China

[6] Tsinghua Univ, Dept Chem, Beijing 100084, Peoples R China

来源：

BIOMATERIALS | 2011年 / 32卷 / 02期

基金：

中国国家自然科学基金;

关键词：

Blood-brain barrier; PAMAM dendrimer; Dual targeting; Drug delivery; Brain cancer; IN-VITRO; PLGA NANOPARTICLES; ENDOTHELIAL-CELLS; DRUG TRANSPORT; DELIVERY; BARRIER; TRANSFERRIN; LIPOSOMES; RECEPTOR; METHOTREXATE;

D O I：

10.1016/j.biomaterials.2010.09.002

中图分类号：

R318 [生物医学工程];

学科分类号：

100103 [病原生物学];

摘要：

A dual-targeting drug carrier (PAMAM-PEG-WGA-Tf) based on the PEGylated fourth generation (G = 4 0) PAMAM dendrimer with transferrin (Tf) and wheat germ agglutinin (WGA) on the periphery and doxorubicin (DOX) loaded in the interior was synthesized and its BBB penetration and tumor targeting properties were explored DLS and TEM measurements revealed the size of PAMAM-PEG-WGA-Tf was in the range of 14-20 nm It reduced the cytotoxicity of DOX to the normal cells greatly while efficiently inhibited the growth rate of the C6 glioma cells The assay of transport across the BBB showed that PAMAM-PEG-WGA-Tf delivered 13 5% of DOX in a period of 2 h demonstrating an enhanced transport ratio as compared to the ratio of 8% for PAMAM-PEG-WGA 7% for PAMAM-PEG-Tf and 5% for free DOX in the same period of time The accumulation of DOX in the tumor site was increased due to the targeting effects of both Tf and WGA leading to the complete breakage of the avascular C6 glioma spheroids in vitro (C) 2010 Elsevier Ltd All rights reserved

引用

页码：478 / 487

页数：10

共 51 条

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Glycoconjugated peptide dendrimers-based nanoparticulate system for the delivery of chloroquine phosphate [J].