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A Smart Drug Delivery System from Charge‐ C onversion Polymer– D rug Conjugate for Enhancing Tumor Therapy and Tunable Drug Release
Author(s) -
Huang Hailong,
Li Yapeng,
Sa Zongpeng,
Sun Yuan,
Wang Yuzhen,
Wang Jingyuan
Publication year - 2014
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201300337
Subject(s) - conjugate , linker , chemistry , drug delivery , drug , intracellular , combinatorial chemistry , extracellular , cytotoxicity , targeted drug delivery , biophysics , drug carrier , hydrazone , pharmacology , stereochemistry , biochemistry , organic chemistry , medicine , in vitro , biology , mathematical analysis , mathematics , computer science , operating system
A smart drug delivery system is prepared by citraconylated polyaspartic acid (PASP) derivate–drug conjugate. The conjugate contains two pH‐sensitive groups: citraconic amide and hydrazone linker. Citraconic amide group can enhance tumor therapy efficiency by the extracellular pH‐sensitive charge‐conversion property. Hydrazone linker between polymer and drug can cleave efficiently in the intracellular pH environment. The resulting conjugate shows dual‐pH sensitive properties: extracellular pH‐triggered enhanced tumor targeting and intracellular pH‐triggered drug release. The results of physicochemical properties, intracellular location, and cytotoxicity of conjugate micelles demonstrate that this novel smart drug delivery system can enhance intracellular delivery of drug at a low pH and then release drug rapidly.