PMID- 30771583 OWN - NLM STAT- MEDLINE DCOM- 20190909 LR - 20190909 IS - 1873-4367 (Electronic) IS - 0927-7765 (Linking) VI - 177 DP - 2019 May 1 TI - Polymeric prodrug microspheres with tumor intracellular microenvironment bioreducible degradation, pH-triggered "off-on" fluorescence and drug release for precise imaging-guided diagnosis and chemotherapy. PG - 313-320 LID - S0927-7765(19)30076-1 [pii] LID - 10.1016/j.colsurfb.2019.02.002 [doi] AB - 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. CI - Copyright (c) 2019 Elsevier B.V. All rights reserved. FAU - Pei, Mingliang AU - Pei M AD - State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, People's Republic of China. FAU - Li, Guoping AU - Li G AD - State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, People's Republic of China. FAU - Ma, Kangwei AU - Ma K AD - State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, People's Republic of China. FAU - Li, Jianan AU - Li J AD - State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, People's Republic of China. FAU - Wang, Yuanfan AU - Wang Y AD - State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, People's Republic of China. FAU - Liu, Peng AU - Liu P AD - State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, People's Republic of China. Electronic address: pliu@lzu.edu.cn. LA - eng PT - Journal Article DEP - 20190204 PL - Netherlands TA - Colloids Surf B Biointerfaces JT - Colloids and surfaces. B, Biointerfaces JID - 9315133 RN - 0 (Antibiotics, Antineoplastic) RN - 0 (Polymers) RN - 0 (Prodrugs) RN - 80168379AG (Doxorubicin) SB - IM MH - Antibiotics, Antineoplastic/chemistry/*pharmacology MH - Apoptosis/drug effects MH - Cell Proliferation/drug effects MH - Cell Survival/drug effects MH - Doxorubicin/chemistry/*pharmacology MH - Drug Liberation MH - Drug Screening Assays, Antitumor MH - Fluorescence MH - Hep G2 Cells MH - Humans MH - Hydrogen-Ion Concentration MH - Microspheres MH - Molecular Structure MH - Particle Size MH - Polymers/*chemistry MH - Prodrugs/*chemistry MH - Surface Properties MH - Tumor Microenvironment/*drug effects OTO - NOTNLM OT - Leakage-free OT - Polymeric prodrug microspheres OT - Precise imaging-guided diagnosis and chemotherapy OT - pH-triggered drug release OT - pH-triggered fluorescence EDAT- 2019/02/17 06:00 MHDA- 2019/09/10 06:00 CRDT- 2019/02/17 06:00 PHST- 2018/10/11 00:00 [received] PHST- 2019/01/29 00:00 [revised] PHST- 2019/02/03 00:00 [accepted] PHST- 2019/02/17 06:00 [pubmed] PHST- 2019/09/10 06:00 [medline] PHST- 2019/02/17 06:00 [entrez] AID - S0927-7765(19)30076-1 [pii] AID - 10.1016/j.colsurfb.2019.02.002 [doi] PST - ppublish SO - Colloids Surf B Biointerfaces. 2019 May 1;177:313-320. doi: 10.1016/j.colsurfb.2019.02.002. Epub 2019 Feb 4.