Hyperbranched Polyphosphates for Drug Delivery Application: Design, Synthesis, and In Vitro Evaluation
writer：Liu, J.Y.; Pang, Y.; Huang, W.*; Zhu, X.Y.; Zhou, Y. F.; Yan, D.Y.*
keywords：Hyperbranched Polyphosphates,Drug Delivery,In Vitro Evaluation
source：期刊
specific source：Biomacromolecules 2010, 11, 1564. http://pubs.acs.org/doi/pdf/10.1021/bm100188h
Issue time：2010年
A water-soluble hyperbranched polyphosphate (HPHEEP) was synthesized
through the self-condensation ring-opening polymerization (SCROP) of
2-(2-hydroxyethoxy)ethoxy-2-oxo-1,3,2-dioxaphospholane (HEEP), and its
suitability as a drug carrier was then evaluated in vitro. Methyl
tetrazolium (MTT) and live/dead staining assays indicated that HPHEEP
had excellent biocompatibility against COS-7 cells. The good
biodegradability of HPHEEP was observed by NMR analysis, and the
degradation products were nontoxic to COS-7 cells. Flow cytometry and
confocal laser scanning microscopy analyses suggested that HPHEEP could
be easily internalized by vivid cells and preferentially accumulated in
the perinuclear region. Furthermore, a hydrophobic anticancer drug,
chlorambucil, was used as a model drug and covalently bound to HPHEEP.
The chlorambucil dose of the conjugate and free drug required for 50%
cellular growth inhibition were 75 and 50 μg/mL, respectively, according
to MTT assay against an MCF-7 breast cancer cell line in vitro. This
high activity of the conjugate may be attributed to the biodegradability
of HPHEEP so as to release the chlorambucil in cells. Therefore, on the
basis of its biocompatibility and biodegradability, HPHEEP could
provide a charming opportunity to design some excellent drug delivery
systems for therapeutic applications.