title: Improving physicochemical properties and doxorubicin cytotoxicity of novel polymeric micelles by poly(ε-caprolactone) segments.
abstract: This study constructed a series of novel micelles based on star-shaped amphiphilic copolymers (sPEC/CDs), and aimed to confirm the important role poly(ε-caprolactone) (PCL) segments played to improve the various properties of micelles. sPEC/CDs, consisting of β-cyclodextrin (β-CD) as a core and monomethoxy poly(ethylene glycol) (mPEG) and PCL diblock copolymers as arms, were synthesized by arm-first method. The critical micelle concentrations (CMC) of sPEC/CDs were determined by fluorescence spectrophotometry using pyrene as a probe. 3-(4, 5-dimethylthiazol-2-yl)- 2,5-diphenyltetrazolium bromide and flow cytometry were used to detect drug cytotoxicity and cellular uptake of the doxorubicin-loaded micelles. Rhodamine-123 cellular accumulation was examined to evaluate the polymer action to P-glycoprotein. It was revealed that, once PCL segment was inserted between β-CD and mPEG, the CMC can be significantly decreased, the drug loading capability greatly improved, and the drug resistance of MCF-7/ADR cells effectively reversed. These findings suggest that sPEC/CDs own potential superiority for cancer therapy as drug carriers.
authors.affiliation: College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China. lyqiu@zju.edu.cn
authors.forename: Liyan
authors.initials: L
authors.lastname: Qiu
authors.forename: Lu
authors.initials: L
authors.lastname: Zhang
authors.forename: Cheng
authors.initials: C
authors.lastname: Zheng
authors.forename: Rongjuan
authors.initials: R
authors.lastname: Wang
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry*; D005434:Flow Cytometry; D006801:Humans; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D015394:Molecular Structure; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D012995:Solubility; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D000903:Antibiotics, Antineoplastic; D004337:Drug Carriers; D008823:Micelles; D011091:Polyesters; D013501:Surface-Active Agents; D047392:beta-Cyclodextrins; C016240:polycaprolactone; D011092:Polyethylene Glycols; D004317:Doxorubicin; C028210:monomethoxypolyethylene glycol; C031215:betadex