The preparation and study on drug release of a triply-responsive (redox/thermo/pH) cross-linked polymeric micelle as anti-cancer drug carrier.
10.7507/1001-5515.201708038
- Author:
Jing QU
1
;
Kanglong CHEN
1
;
Qiuyue WANG
1
;
Juan LIN
2
;
Qinghan ZHOU
3
Author Information
1. School of Chemical & Environmental Protection Engineering, Southwest Minzu University, Chengdu 610041, P.R.China.
2. School of Biomedical Science, Chengdu Medical College, Chengdu 610083, P.R.China.
3. School of Chemical & Environmental Protection Engineering, Southwest Minzu University, Chengdu 610041, P.R.China.zhqinghan@163.com.
- Publication Type:Journal Article
- Keywords:
cross-linked polymeric micelle;
drug release;
pH-sensitivity;
redox-sensitivity;
temperature-sensitivity
- From:
Journal of Biomedical Engineering
2018;35(1):70-80
- CountryChina
- Language:Chinese
-
Abstract:
A multiple-stimuli-responsive drug-conjugated cross-linked micelles was prepared by radical copolymerization. The chemical structure, morphology, and size of the cross-linked micelles were characterized, and the drug loading of the micelle was calculated. The experimental results indicated that the hydrodynamic size of the drug-loaded micelles were about 100 nm, and the as prepared micelles could be degraded and swelled in presence of reducing glutathione (GSH). The low critical solution temperature (LCST) of the micelle was around 39.4℃. According to the experimental results, the micelles will shrink at temperature above the LCST. Subsequently, the accumulative drug release rate was up to 91.78% under acidic (pH 5.0), reductive (GSH 10 mmol/L) and high temperature (42.0℃) conditions mimicking the tumor microenvironment, while a relatively low release rate of 1.12% was observed without stimulation. The drug-conjugated cross-linked micelles showed a strong cell uptake behavior. In the cytotoxicity assay, the micelles exhibited effective anti-cancer activity and excellent biocompatibility. In brief, the experimental results show that the as-prepared drug-conjugated cross-linked micelle exhibits multiple stimuli-responsiveness, which holds great promise for anti-cancer drug delivery.