Polymeric prodrug microspheres with tumor intracellular microenvironment bioreducible degradation, pH-triggered "off-on" fluorescence and drug release for precise imaging-guided diagnosis and chemotherapy.
Colloids Surf B Biointerfaces
; 177: 313-320, 2019 May 01.
Article
en En
| MEDLINE
| ID: mdl-30771583
ABSTRACT
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.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Polímeros
/
Profármacos
/
Doxorrubicina
/
Microambiente Tumoral
/
Antibióticos Antineoplásicos
Tipo de estudio:
Diagnostic_studies
Límite:
Humans
Idioma:
En
Revista:
Colloids Surf B Biointerfaces
Asunto de la revista:
QUIMICA
Año:
2019
Tipo del documento:
Article