title: Self-assembly of phospholipid-analogous hyperbranched polymers nanomicelles for drug delivery.
abstract: A drug nanocarrier has been constructed through self-assembly of phospholipid analogous hyperbranched polymers (HPHEEP-alkyls) which contain a polar hyperbranched polyphosphate headgroup and many aliphatic tails. HPHEEP-alkyls were synthesized by self-condensing ring-opening polymerization of 2-(2-hydroxyethoxy)ethoxy-2-oxo-1,3,2-dioxaphospholane and then capped with palmitoyl chloride. Benefiting from the amphiphilic structure with the hydrophilic core and many hydrophobic tails, HPHEEP-alkyls were able to self-assemble into nanomicelles in aqueous media. Importantly, the size of the nanomicelles could be controlled conveniently from 98 to 215 nm by adjusting the capped fraction of the hydroxyl groups with hydrophobic palmityls. The excellent biocompatibility of these nanomicelles was confirmed by methyl tetrazolium assay and acridine orange/ethidium bromide double staining against COS-7 cells. Confocal laser scanning microscopy and flow cytometry analysis demonstrated their good cell permeability, i.e. these nanomicelles were easily internalized by vivid cells and mainly located in the cytoplasm rather than nucleolus. Chlorambucil-loaded nanomicelles were investigated for proliferation inhibition of a MCF-7 breast cancer cell line in vitro, and the chlorambucil dose required for 50% cellular growth inhibition was found to be 5 microg/mL. All of these results indicate that HPHEEP-alkyls nanomicelles can be used as safe and promising drug nanocarriers.
authors.affiliation: School of Chemistry and Chemical Engineering, State Key Laboratory of Metal Matrix Composites, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai, 200240, PR China.
authors.forename: Jinyao
authors.initials: J
authors.lastname: Liu
authors.forename: Yan
authors.initials: Y
authors.lastname: Pang
authors.forename: Wei
authors.initials: W
authors.lastname: Huang
authors.forename: Xinyuan
authors.initials: X
authors.lastname: Zhu
authors.forename: Yongfeng
authors.initials: Y
authors.lastname: Zhou
authors.forename: Deyue
authors.initials: D
authors.lastname: Yan
mesh_terms: D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D003460:Crystallization / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D008422:Materials Testing; D008823:Micelles; D053758:Nanoparticles / Q000737:chemistry* / Q000627:therapeutic use* / Q000648:ultrastructure; D010743:Phospholipids / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry*; D016896:Treatment Outcome
chemical_list: D004337:Drug Carriers; D008823:Micelles; D010743:Phospholipids; D011108:Polymers