title: Construction and application of biotin-poloxamer conjugate micelles for chemotherapeutics.
abstract: Biotin was conjugated on poloxamer to prepare biotin-poloxamer (BP) conjugate micelles for chemotherapeutics. Epirubicin (EPI) was encapsulated in BP micelles. The EPI-loaded BP micelles were characterized in terms of size, ζ-potential, morphology, drug loading, drug encapsulation and drug release. Marrow leukemic HL-60 cells were used for evaluating the in vitro cytotoxicity of EPI-loaded BP micelles. Nude mice were axillainoculated subcutaneously HL-60 cells to establish tumour model for investigating the inhibition effects of EPI-loaded BP micelles. From the results, the sizes of these nanoparticles were about 100 nm. Fluorescence microscope observation supported the enhanced cellular uptake of the micelles. The order of the inhibition on tumour volume growth was: EPI-loaded BP micelles >EPI-loaded MATP micelles >EPI-loaded poloxamer micelles >EPI. BP micelles showed significant antitumour activity and low toxicity, compared with the non-targeted micelles. With the advantage of EPR effect and tumour-targeting potential, BP conjugate micelles might be developed as a new system for chemotherapeutics.
authors.affiliation: Department of Pharmacy, The Second Affiliated Hospital of Wenzhou Medical College, Zhejiang Province 325027, Wenzhou City, China.
authors.forename: Guang-Yong
authors.initials: GY
authors.lastname: Lin
authors.forename: Hai-Feng
authors.initials: HF
authors.lastname: Lv
authors.forename: Cui-Tao
authors.initials: CT
authors.lastname: Lu
authors.forename: Li-Juan
authors.initials: LJ
authors.lastname: Chen
authors.forename: Min
authors.initials: M
authors.lastname: Lin
authors.forename: Ming
authors.initials: M
authors.lastname: Zhang
authors.forename: Ying-Zheng
authors.initials: YZ
authors.lastname: Zhao
authors.forename: Zheng-Xing
authors.initials: ZX
authors.lastname: Su
authors.forename: Xiao-Tong
authors.initials: XT
authors.lastname: Shen
authors.forename: Xi
authors.initials: X
authors.lastname: Jiang
authors.forename: Rong-Rong
authors.initials: RR
authors.lastname: Jin
authors.forename: Xin
authors.initials: X
authors.lastname: Li
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D001710:Biotin / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D015251:Epirubicin / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D018922:HL-60 Cells; D006801:Humans; D008297:Male; D051379:Mice; D008819:Mice, Nude; D008823:Micelles; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D020442:Poloxamer / Q000737:chemistry*
chemical_list: D000903:Antibiotics, Antineoplastic; D004337:Drug Carriers; D008823:Micelles; D020442:Poloxamer; D015251:Epirubicin; D001710:Biotin