Details

Autor(en) / Beteiligte

• Pei, Mingliang
• Jia, Xu
• Li, Guoping
• Liu, Peng

Titel

Versatile Polymeric Microspheres with Tumor Microenvironment Bioreducible Degradation, pH-Activated Surface Charge Reversal, pH-Triggered “off–on” Fluorescence and Drug Release as Theranostic Nanoplatforms

Ist Teil von

• Molecular pharmaceutics, 2019-01, Vol.16 (1), p.227-237

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2019

Link zum Volltext

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• Facile approach has been developed for the versatile polymeric microspheres with tumor microenvironment bioreducible degradation, pH-activated surface charge reversal, pH-triggered “off-on” fluorescence, and drug release via emulsion copolymerization of glycidyl methacrylate (GMA), poly­(ethylene glycol) methyl ether methacrylate (PEGMA), and N-rhodamine 6G-ethyl-acrylamide (Rh6GEAm) with N,N-bis­(acyloyl)­cystamine) (BACy) as disulfide cross-linker and functionalization. The final PGMA-DMMA microspheres showed excellent cytocompatibility, pH-triggered surface charge reversal at pH 5–6, strong fluorescence only in acidic media, and bioreducible degradation with high reductant level, indicating their promising application as theranostic nanoplatforms for precise imaging-guided diagnosis and chemotherapy. The DOX-loaded PGMA-DMMA microspheres with a drug-loading capacity of 18% and particle size of about 150 nm possessed unique pH/reduction dual-responsive controlled release, with a cumulative DOX release of 60.5% within 54 h at the simulated tumor microenvironment but a premature leakage of <8.0% under the simulated physiological condition. Enhanced inhibition efficacy against HepG2 cells was achieved compared to free DOX.