PMID- 32090637 OWN - NLM STAT- MEDLINE DCOM- 20201127 LR - 20210423 IS - 1521-0464 (Electronic) IS - 1071-7544 (Print) IS - 1071-7544 (Linking) VI - 27 IP - 1 DP - 2020 Dec TI - Bicomponent polymeric micelles for pH-controlled delivery of doxorubicin. PG - 344-357 LID - 10.1080/10717544.2020.1726526 [doi] AB - Stimuli-responsive drug delivery systems (DDSs) are expected to realize site-specific drug release and kill cancer cells selectively. In this study, a pH-responsive micelle was designed utilizing the pH-sensitivity of borate bonds formed between dopamine and boronic acid. First, methyl (polyethylene glycol)-block-polycaprolactone (mPEG-PCL) was conjugated with 4-cyano-4-(thiobenzoylthio)pentanoic acid (CTP) to obtain a macroinitiator. Two different segments poly(dopamine methacrylamide) (PDMA) and poly(vinylphenylboronic acid) (PVBA) were then grafted to the end of mPEG-PCL. Two triblock copolymers, mPEG-PCL-PDMA and mPEG-PCL-PVBA, were then obtained by reversible addition-fragmentation transfer (RAFT) polymerization. These copolymers and their mixture self-assembled in aqueous solution to form micelles that were able to load hydrophobic anticancer drug doxorubicin (DOX). These two-component micelles were found to be pH-sensitive, in contrast to the one-component micelles. Furthermore, MTT studies showed that the micelles were almost nontoxic. The DOX-loaded micelles showed cytotoxicity equivalent to that of DOX at high concentration. In vivo antitumor experiments showed that this pH-sensitive polymeric micellar system had an enhanced therapeutic effect on tumors. These two-component boronate-based pH micelles are universally applicable to the delivery of anticancer drugs, showing great potential for cancer therapy. FAU - Wang, Chunyun AU - Wang C AD - Institute of Pharmacy, School of Pharmacy, Henan University, Kaifeng, China. FAU - Qi, Peilan AU - Qi P AD - Institute of Pharmacy, School of Pharmacy, Henan University, Kaifeng, China. FAU - Lu, Yan AU - Lu Y AD - Institute of Pharmacy, School of Pharmacy, Henan University, Kaifeng, China. FAU - Liu, Lei AU - Liu L AD - Institute of Pharmacy, School of Pharmacy, Henan University, Kaifeng, China. FAU - Zhang, Yanan AU - Zhang Y AD - Institute of Pharmacy, School of Pharmacy, Henan University, Kaifeng, China. FAU - Sheng, Qianli AU - Sheng Q AD - Institute of Pharmacy, School of Pharmacy, Henan University, Kaifeng, China. FAU - Wang, Tianshun AU - Wang T AD - Institute of Pharmacy, School of Pharmacy, Henan University, Kaifeng, China. FAU - Zhang, Mengying AU - Zhang M AD - Institute of Pharmacy, School of Pharmacy, Henan University, Kaifeng, China. FAU - Wang, Rui AU - Wang R AD - Institute of Pharmacy, School of Pharmacy, Henan University, Kaifeng, China. FAU - Song, Shiyong AU - Song S AUID- ORCID: 0000-0003-2208-608X AD - Institute of Pharmacy, School of Pharmacy, Henan University, Kaifeng, China. LA - eng PT - Journal Article PL - England TA - Drug Deliv JT - Drug delivery JID - 9417471 RN - 0 (Antibiotics, Antineoplastic) RN - 0 (Boronic Acids) RN - 0 (Drug Carriers) RN - 0 (Micelles) RN - 0 (Polymers) RN - 80168379AG (Doxorubicin) SB - IM MH - Animals MH - Antibiotics, Antineoplastic/*administration & dosage/chemistry/pharmacology MH - Boronic Acids/chemistry MH - Doxorubicin/*administration & dosage/chemistry/pharmacology MH - Drug Carriers/chemistry MH - *Drug Delivery Systems MH - Drug Liberation MH - Female MH - Humans MH - Hydrogen-Ion Concentration MH - Mice MH - Micelles MH - Neoplasms/drug therapy MH - Polymers/*chemistry MH - Xenograft Model Antitumor Assays PMC - PMC7054969 OTO - NOTNLM OT - Drug delivery OT - boronate ester OT - cancer OT - micelle OT - pH-responsive EDAT- 2020/02/25 06:00 MHDA- 2020/11/28 06:00 PMCR- 2020/02/24 CRDT- 2020/02/25 06:00 PHST- 2020/02/25 06:00 [entrez] PHST- 2020/02/25 06:00 [pubmed] PHST- 2020/11/28 06:00 [medline] PHST- 2020/02/24 00:00 [pmc-release] AID - 1726526 [pii] AID - 10.1080/10717544.2020.1726526 [doi] PST - ppublish SO - Drug Deliv. 2020 Dec;27(1):344-357. doi: 10.1080/10717544.2020.1726526.