PMID- 27883931 OWN - NLM STAT- MEDLINE DCOM- 20170328 LR - 20180115 IS - 1873-4367 (Electronic) IS - 0927-7765 (Linking) VI - 150 DP - 2017 Feb 1 TI - Disassembly of amphiphilic small molecular prodrug with fluorescence switch induced by pH and folic acid receptors for targeted delivery and controlled release. PG - 50-58 LID - S0927-7765(16)30802-5 [pii] LID - 10.1016/j.colsurfb.2016.11.021 [doi] AB - We develop a new type of pH-responsive amphiphilic small molecular prodrug by conjugating folic acid with anti-tumour doxorubicin via a hydrazone bond. This prodrug is featured by high and precise drug loading (55.4wt%), which can self-assemble into micellar nanoparticles in neutral environment while disassemble in the presence of tumour cells expressing folic acid receptors or the acidic tumoral endosomal environment. The prodrug nanoparticles can effectively improve anticancer efficacy due to the features of pH-triggered drug release and targeted delivery. Moreover, in vitro cell study further indicated that the resulting prodrug nanoparticles had enhanced cytotoxicity for folic-acid-positive cells (HeLa) compared to folic-acid-negative cells (MCF-7). More importantly, the induced disassembly of prodrug nanoparticles can "switch on" the inherent fluorescence of the internalized doxorubicin drug in the tumour microenvironment, which can be used for the detection of tumour cells. We believe that this strategy can pave a new way for designing small molecular drug delivery systems and facilitate tumour diagnosis and treatment simultaneously. CI - Copyright (c) 2016 Elsevier B.V. All rights reserved. FAU - Xu, Zhigang AU - Xu Z AD - Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University, Chongqing 400715, PR China; Chongqing Key Laboratory for Advanced Materials and Technologies of Clean Energies, Chongqing 400715, PR China. Electronic address: zgxu@swu.edu.cn. FAU - Shi, Xiaoxiao AU - Shi X AD - Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University, Chongqing 400715, PR China; Chongqing Key Laboratory for Advanced Materials and Technologies of Clean Energies, Chongqing 400715, PR China. FAU - Hou, Meili AU - Hou M AD - Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University, Chongqing 400715, PR China; Chongqing Key Laboratory for Advanced Materials and Technologies of Clean Energies, Chongqing 400715, PR China. FAU - Xue, Peng AU - Xue P AD - Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University, Chongqing 400715, PR China; Chongqing Key Laboratory for Advanced Materials and Technologies of Clean Energies, Chongqing 400715, PR China. FAU - Gao, Yong-E AU - Gao YE AD - Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University, Chongqing 400715, PR China; Chongqing Key Laboratory for Advanced Materials and Technologies of Clean Energies, Chongqing 400715, PR China. FAU - Liu, Shiying AU - Liu S AD - School of Chemical and Biomedical Engineering, Nanyang Technological University, 62 Nanyang Drive, Singapore 637459, Singapore. FAU - Kang, Yuejun AU - Kang Y AD - Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University, Chongqing 400715, PR China; Chongqing Key Laboratory for Advanced Materials and Technologies of Clean Energies, Chongqing 400715, PR China. Electronic address: yjkang@swu.edu.cn. LA - eng PT - Journal Article DEP - 20161117 PL - Netherlands TA - Colloids Surf B Biointerfaces JT - Colloids and surfaces. B, Biointerfaces JID - 9315133 RN - 0 (Antineoplastic Agents) RN - 0 (Delayed-Action Preparations) RN - 0 (Folate Receptors, GPI-Anchored) RN - 0 (Hydrazones) RN - 0 (Micelles) RN - 0 (Prodrugs) RN - 80168379AG (Doxorubicin) RN - 935E97BOY8 (Folic Acid) SB - IM MH - Antineoplastic Agents/chemistry MH - Delayed-Action Preparations/chemistry MH - Doxorubicin/chemistry MH - *Drug Delivery Systems MH - Endosomes/metabolism MH - Fluorescence MH - Folate Receptors, GPI-Anchored/*chemistry MH - Folic Acid/*chemistry MH - HeLa Cells MH - Humans MH - Hydrazones/chemistry MH - Hydrogen-Ion Concentration MH - MCF-7 Cells MH - Magnetic Resonance Spectroscopy MH - Micelles MH - Nanoparticles/chemistry MH - Prodrugs/*chemistry MH - *Spectrometry, Fluorescence OTO - NOTNLM OT - Cancer therapy OT - Controlled release OT - Diagnosis OT - Drug delivery OT - Small molecular prodrug EDAT- 2016/11/25 06:00 MHDA- 2017/03/30 06:00 CRDT- 2016/11/25 06:00 PHST- 2016/09/03 00:00 [received] PHST- 2016/11/08 00:00 [revised] PHST- 2016/11/16 00:00 [accepted] PHST- 2016/11/25 06:00 [pubmed] PHST- 2017/03/30 06:00 [medline] PHST- 2016/11/25 06:00 [entrez] AID - S0927-7765(16)30802-5 [pii] AID - 10.1016/j.colsurfb.2016.11.021 [doi] PST - ppublish SO - Colloids Surf B Biointerfaces. 2017 Feb 1;150:50-58. doi: 10.1016/j.colsurfb.2016.11.021. Epub 2016 Nov 17.