PMID- 25661387 OWN - NLM STAT- MEDLINE DCOM- 20151015 LR - 20220318 IS - 1950-6007 (Electronic) IS - 0753-3322 (Linking) VI - 69 DP - 2015 Feb TI - Soluplus((R)) micelles as a potential drug delivery system for reversal of resistant tumor. PG - 388-95 LID - S0753-3322(14)00223-6 [pii] LID - 10.1016/j.biopha.2014.12.028 [doi] AB - Inhibiting or circumventing drug resistance by using drug delivery systems (DDSs) such as micelles has attracted significant attention recently. In this present study, a polyvinyl caprolactam-polyvinyl acetate-polyethylene (Soluplus((R))) micelle was developed as the delivery system for doxorubicin (DOX) and evaluated both in vitro and in vivo. In vitro, Soluplus((R)) micelles could significantly enhance the cellular accumulation of DOX in MCF-7/DOX cells, meanwhile, P-glycoprotein (P-gp)-mediated drug efflux was inhibited which was also verified in the membrane fluidity study. And MCF-7/DOX cells were found to be more susceptible to the cytotoxic effects of DOX-M. In vivo, both the P-gp inhibitors verapamil and Soluplus((R)) could improve the cytotoxicity of DOX.HCl in MCF-7/DOX tumor-bearing mice, which were further certified by the effect of Soluplus((R)) on P-gp inhibition. Furthermore, the excellent antitumor efficacy of DOX-M by intravenous injection was also observed, which indicated that the P-gp inhibition effect of Soluplus((R)) could enhance the susceptibility of resistant tumor to DOX in vivo. In conclusion, our study suggested that Soluplus((R)) micelles might be an applicable drug delivery system for enhancing the antitumor efficacy of P-gp substrates. CI - Crown Copyright (c) 2014. Published by Elsevier Masson SAS. All rights reserved. FAU - Jin, Xiang AU - Jin X AD - College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310032, PR China. Electronic address: jinxiangzjut@hotmail.com. FAU - Zhou, Bo AU - Zhou B AD - Jiangsu Center of Safety Evaluation for Drugs, School of Pharmaceutical Sciences, Nanjing University of Technology, Nanjing 210009, PR China. FAU - Xue, Lezhen AU - Xue L AD - Jiangsu Center of Safety Evaluation for Drugs, School of Pharmaceutical Sciences, Nanjing University of Technology, Nanjing 210009, PR China. FAU - San, Weiguang AU - San W AD - College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310032, PR China. LA - eng PT - Journal Article DEP - 20141224 PL - France TA - Biomed Pharmacother JT - Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie JID - 8213295 RN - 0 (ATP Binding Cassette Transporter, Subfamily B, Member 1) RN - 0 (Antineoplastic Agents) RN - 0 (Micelles) RN - 0 (Polyvinyls) RN - 0 (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer) RN - 3WJQ0SDW1A (Polyethylene Glycols) RN - 80168379AG (Doxorubicin) SB - IM MH - ATP Binding Cassette Transporter, Subfamily B, Member 1/antagonists & inhibitors/metabolism MH - Animals MH - Antineoplastic Agents/pharmacology MH - Doxorubicin/pharmacology MH - *Drug Delivery Systems MH - *Drug Resistance, Neoplasm/drug effects MH - Endocytosis/drug effects MH - Female MH - Hep G2 Cells MH - Humans MH - Inhibitory Concentration 50 MH - Kinetics MH - MCF-7 Cells MH - Mice, Inbred BALB C MH - Mice, Nude MH - *Micelles MH - Polyethylene Glycols/*chemistry MH - Polyvinyls/*chemistry OTO - NOTNLM OT - Antitumor efficacy OT - Doxorubicin OT - P-glycoprotein OT - Soluplus((R)) micelle EDAT- 2015/02/11 06:00 MHDA- 2015/10/16 06:00 CRDT- 2015/02/10 06:00 PHST- 2014/11/25 00:00 [received] PHST- 2014/12/11 00:00 [accepted] PHST- 2015/02/10 06:00 [entrez] PHST- 2015/02/11 06:00 [pubmed] PHST- 2015/10/16 06:00 [medline] AID - S0753-3322(14)00223-6 [pii] AID - 10.1016/j.biopha.2014.12.028 [doi] PST - ppublish SO - Biomed Pharmacother. 2015 Feb;69:388-95. doi: 10.1016/j.biopha.2014.12.028. Epub 2014 Dec 24.