N-Boc-Histidine-Capped PLGA-PEG-PLGA as a Smart Polymer for Drug Delivery Sensitive to Tumor Extracellular pH

被引：74

作者：

Chang, Guangtao ^{[1
]}

Li, Chong ^{[2
]}

Lu, Weiyue ^{[2
]}

Ding, Jiandong ^{[1
]}

机构：

[1] Fudan Univ, Key Lab Mol Engn Polymers Minist Educ, Dept Macromol Sci, Adv Mat Lab, Shanghai 200433, Peoples R China

[2] Fudan Univ, Dept Pharmaceut, Sch Pharm, Shanghai 201203, Peoples R China

来源：

MACROMOLECULAR BIOSCIENCE | 2010年 / 10卷 / 10期

关键词：

block copolymers; drug delivery systems; micelles; POROUS POLY(D; L-LACTIDE-CO-GLYCOLIDE); SCAFFOLDS; SCORPION-LIKE MACROMOLECULES; BLOCK-COPOLYMER MICELLES; IN-VITRO DEGRADATION; TRIBLOCK COPOLYMERS; DOXORUBICIN; RELEASE; NANOPARTICLES; HYDROGELS; SOL;

D O I：

10.1002/mabi.201000117

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A pH-sensitive polymer was synthesized by introducing the N-Boc-histidine to the ends of a PLGA-PEG-PLGA block copolymer. The synthesized polymer was confirmed to be biodegradable and biocompatible, well dissolved in water and forming micelles above the CMC. DOX was employed as a model anticancer drug. In vitro drug release from micelles of N-Boc-histidine-capped PLGA-PEG-PLGA exhibited significant difference between pH = 6.2 and pH = 7.4, whereas DOX release from micelles composed of un-capped virgin polymers was not significantly sensitive to medium pH. Uptake of DOX from micelles of the new polymer into MDA-MB-435 solid tumor cells was also observed, and pH sensitivity was confirmed. Hence, the N-Boc-histidine capped PLGA-PEG-PLGA might be a promising material for tumor targeting.

引用

页码：1248 / 1256

页数：9

共 49 条

[1] Acid-cleavable polymeric core-shell particles for delivery of hydrophobic drugs [J].

Chan, Yannie ;

Bulmus, Volga ;

Zareie, M. Hadi ;

Byrne, Frances L. ;

Barner, Leonie ;

Kavallaris, Maria .

JOURNAL OF CONTROLLED RELEASE, 2006, 115 (02) :197-207

[2] A delicate ionizable-group effect on self-assembly and thermogelling of amphiphilic block copolymers in water [J].

Chang, Guangtao ;

Yu, Lin ;

Yang, Zigang ;

Ding, Jiandong .

POLYMER, 2009, 50 (25) :6111-6120

[3]

Dean J.A., 2001, Lange's Handbook of Chemistry, V15

[4] Micellar Nanocarriers Assembled from Doxorubicin-Conjugated Amphiphilic Macromolecules (DOX-AM) [J].

del Rosario, Leilani S. ;

Demirdirek, Bahar ;

Harmon, Alexander ;

Orban, David ;

Uhrich, Kathryn E. .

MACROMOLECULAR BIOSCIENCE, 2010, 10 (04) :415-423

[5] Preparation of Multifunctional Drug Carrier for Tumor-Specific Uptake and Enhanced Intracellular Delivery through the Conjugation of Weak Acid Labile Linker [J].

Ding, Caixia ;

Gu, Jingxia ;

Qu, Xiaozhong ;

Yang, Zhenzhong .

BIOCONJUGATE CHEMISTRY, 2009, 20 (06) :1163-1170

[6] Polymeric micelles based on amphiphilic scorpion-like macromolecules: Novel carriers for water-insoluble drugs [J].

Djordjevic, J ;

Barch, M ;

Uhrich, KE .

PHARMACEUTICAL RESEARCH, 2005, 22 (01) :24-32

[7] Amphiphilic Scorpion-like Macromolecules as Micellar Nanocarriers [J].

Djordjevic, Jelena ;

Del Rosario, Leilani S. ;

Wang, Jinzhong ;

Uhrich, Kathryn E. .

JOURNAL OF BIOACTIVE AND COMPATIBLE POLYMERS, 2008, 23 (06) :532-551

[8] PH-responsive self-assembly of carboxyl-terminated hyperbranched polymers [J].

Dong, Wenyong ;

Zhou, Yongfeng ;

Yan, Deyue ;

Li, Huiqin ;

Liu, Yu .

PHYSICAL CHEMISTRY CHEMICAL PHYSICS, 2007, 9 (10) :1255-1262

[9]

Etrych T, 2002, MACROMOL BIOSCI, V2, P43, DOI 10.1002/1616-5195(20020101)2:1<43::AID-MABI43>3.0.CO

[10]

2-8

← 1 2 3 4 5 →