An Acid-Triggered Degradable and Fluorescent Nanoscale Drug Delivery System with Enhanced Cytotoxicity to Cancer Cells.

Abstract

To reduce side-effects of anticancer drugs, development of nanocarriers with precise biological functions is a critical requirement. In this study, the multifunctional nanoparticles combining imaging and therapy for tumor-targeted delivery of hydrophobic anticancer drugs were prepared via self-assembly of amphiphilic copolymers obtained using RAFT polymerization, specifically, acid-labile ortho ester and galactose. First, boron-dipyrromethene dye-conjugated chain transfer agent provides fluorescent imaging capability for diagnostic application. Second, nanoparticles were stable under physiological conditions but degraded in acidic tumor microenvironment, leading to enhanced anticancer efficacy. Third, the application of biocompatible glycopolymers efficiently increased the target-to-background ratio through carbohydrate-protein interactions. Data from cell viability, cellular internalization, flow cytometry, biodistribution and anticancer efficacy tests showed that the drug-loaded nanoparticles were capable of inhibiting cancer cell proliferation with significantly enhanced capacity. Our newly developed multifunctional nanoparticles may thus facilitate the development of effective drug delivery systems for application in diagnosis and therapy of cancer.

• Authors: Jinxia An, Xiaomei Dai, Zhongming Wu, Yu Zhao, Zhentan Lu, Qianqian Guo, Xinge Zhang, Chaoxing Li
• Journal: Biomacromolecules (Biomacromolecules) Vol. 16 Issue 8 Pg. 2444-54 (Aug 10 2015) ISSN: 1526-4602 [Electronic] United States
• PMID: 26213802 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Drug Carriers
• Polymers
• Doxorubicin

Topics

• Antineoplastic Agents (administration & dosage, chemistry)
• Cell Proliferation (drug effects)
• Cell Survival (drug effects)
• Doxorubicin (administration & dosage, chemistry)
• Drug Carriers (administration & dosage, chemistry)
• Drug Delivery Systems
• HeLa Cells
• Humans
• Hydrophobic and Hydrophilic Interactions
• Nanoparticles (administration & dosage, chemistry)
• Neoplasms (drug therapy)
• Polymers (administration & dosage, chemistry)