Details

Autor(en) / Beteiligte

• Pei, Mingliang
• Li, Guoping
• Ma, Kangwei
• Li, Jianan
• Wang, Yuanfan
• Liu, Peng

Titel

Polymeric prodrug microspheres with tumor intracellular microenvironment bioreducible degradation, pH-triggered “off-on” fluorescence and drug release for precise imaging-guided diagnosis and chemotherapy

Ist Teil von

• Colloids and surfaces, B, Biointerfaces, 2019-05, Vol.177, p.313-320

Ort / Verlag

Netherlands: Elsevier B.V

Erscheinungsjahr

2019

Quelle

Access via ScienceDirect (Elsevier)

Beschreibungen/Notizen

• [Display omitted] •Prodrug nanoparticles were designed for precise imaging-guided diagnosis and chemotherapy.•They showed tumor-microenvironment pH-triggered “off-on” fluorescence and drug release.•But no fluorescence and drug release in physiological medium. Theranostic nanoplatforms have been recognized for imaging-guided diagnosis and chemotherapy of cancer by integrating imaging function into the drug delivery systems (DDSs). Here, a facile approach was developed for the fabrication of polymeric prodrug microspheres by introducing pH sensitive “off-on” fluorochrome Rhodamine 6G into bioreducible cleavable bisulfide crosslinked PEGylated poly(glycidyl methacrylate) (PEG-PGMA) microspheres, followed with chemical conjugation of doxorubicin (DOX) via an acid-labile hydrazone linkage. High drug content of 25.4% was achieved for the final PEG-PGMA-Hy-DOX prodrug microspheres with average hydrodynamic diameter of 332 nm. The in vitro controlled release showed leakage-free in physiological medium but a sustained drug release up to 58% within 56 h in tumor intracellular microenvironment. The cellular experiments showed that the PEG-PGMA-Hy-DOX prodrug microspheres could be effectively internalized into HepG2 cells with enhanced anti-tumor efficacy than the free DOX. Furthermore, they showed fluorescence only in tumor intracellular microenvironment, indicating their promising potential for precise imaging-guided diagnosis and chemotherapy.