Folic acid-Conjugated pH/temperature/redox multi-stimuli responsive biodegradable polymer microspheres for delivery of anti-cancer drugs
writer:Rongrong Li, Fuli Feng, Yinsong Wang, Xiaoying Yang*, Xinlin Yang* and Victor C. Yang
keywords:Folic acid-conjugated; pH/temperature/redox multi-stimuli responsive; Drug delivery; Distillation-precipitation polymerization.
source:期刊
specific source:J Colloid Interface Sci 429 (1), 34-44 (2014). DOI: 10.1016/j.jcis.2014.05.008
Issue time:2014年
The folic
acid (FA)-conjugated pH/temperature/redox multi-stimuli responsive poly(methacrylic
acid-co-N,N-bis(acryloyl)cystamine/poly(N-isopropylacrylamide -co-glycidyl methacrylate-co-N,N-bis(acryloyl)cystamine) microspheres
were prepared by a
two-stage distillation-precipitation polymerization
with subsequent surface modification with FA. The microspheres were
characterized by transmission electron microscopy, dynamical
light scattering, Fourier-transform infrared spectra, UV-vis spectra and elemental analysis. The degradation of the functional microspheres could be triggered by a
reductive reagent, such as glutathione, due to presence of BAC crosslinker. The drug-loaded microspheres exhibited a pH/temperature/redox multi-stimuli responsive drug release character for
doxorubicin hydrochloride as a model anti-cancer drug, which was efficiently loaded into the microspheres with a high
loading capacity of 208.0% and an encapsulation efficiency of 85.4%. In vitro drug delivery study indicated that
the FA-conjugated microspheres could deliver Dox into
MCF-7 cells more efficiently than the microspheres without
functionalization of FA. Furthermore, WST-1 assay showed that the microspheres had no obvious
toxicity to MCF-7 cells even at a high concentration of 2000 μg mL-1. The resultant microsphere may be a promising vector for delivery of anti-cancer drugs as it exhibits a low cytotoxicity and degradability, precise molecular targeting property and multi-stimuli responsively controlled drug release.