Self-Assembly of phospholipid-analogous hyperbranched polymers nanomicelles for drug delivery
writer：Liu, J.Y., Pang, Y.; Huang, W.; Zhu, X.Y., Zhou, Y. F.; Yan, D.Y.
keywords：Nanomicelles, Hyperbranched polyphosphate, Cytotoxicity, Cellular uptake, Drug delivery
source：期刊
specific source：Biomaterials 2010, 31, 1334. http://www.sciencedirect.com/science/article/pii/S0142961209011089
Issue time：2009年
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 μg/mL. All of these
results indicate that HPHEEP-alkyls nanomicelles can be used as safe and
promising drug nanocarriers.