%0 Journal Article
%A Li, Jianfeng
%A Jiang, Xutao
%A Guo, Yubo
%A An, Sai
%A Kuang, Yuyang
%A Ma, Haojun
%A He, Xi
%A Jiang, Chen
%D 2015
%T Linear–Dendritic Copolymer Composed of Polyethylene
Glycol and All-trans-Retinoic Acid as Drug Delivery Platform for Paclitaxel
against Breast Cancer
%U https://acs.figshare.com/articles/journal_contribution/Linear_Dendritic_Copolymer_Composed_of_Polyethylene_Glycol_and_All_trans_Retinoic_Acid_as_Drug_Delivery_Platform_for_Paclitaxel_against_Breast_Cancer/2185099
%R 10.1021/acs.bioconjchem.5b00030.s001
%2 https://acs.figshare.com/ndownloader/files/3819265
%K uptake
%K MRT
%K efficacy
%K NIR
%K CMC
%K tumor accumulation
%K PTX
%K micelle
%K Paclitaxel
%K anticancer drug delivery platform
%K PEG
%K breast cancer treatment
%K Taxol group 24 h postinjection
%K ATRA
%K AUC
%K PDI
%K mg
%K copolymer
%K Drug Delivery Platform
%K concentration
%K MCF
%X A new
linear–dendritic copolymer composed of poly(ethylene
glycol) (PEG) and all-trans-retinoic acid (ATRA) was synthesized as
the anticancer drug delivery platform (PEG-G3-RA8). It
can self-assemble into core–shell micelles with a low critical
micelle concentration (CMC) at 3.48 mg/L. Paclitaxel (PTX) was encapsulated
into PEG-G3-RA8 to form PEG-G3-RA8/PTX micelles
for breast cancer treatment. The optimized formulation had high drug
loading efficacy (20% w/w of drug copolymer ratio), nanosized diameter
(27.6 nm), and narrow distribution (PDI = 0.103). Compared with Taxol,
PEG-G3-RA8/PTX remained highly stable in the serum-containing
cell medium and exhibited 4-fold higher cellular uptake. Besides,
near-infrared fluorescence (NIR) optical imaging results indicated
that fluorescent probe loaded micelle had a preferential accumulation
in breast tumors. Pharmacokinetics and biodistribution studies (10
mg/kg) showed the area under the plasma concentration–time
curve (AUC0‑∞) and mean residence time (MRT0‑∞) for PEG-G3-RA8/PTX and Taxol
were 12.006 ± 0.605 mg/L h, 2.264 ± 0.041 h and 15.966 ±
1.614 mg/L h, 1.726 ± 0.097 h, respectively. The tumor accumulation
of PEG-G3-RA8/PTX group was 1.89-fold higher than that
of Taxol group 24 h postinjection. With the advantages like efficient
cellular uptake and preferential tumor accumulation, PEG-G3-RA8/PTX showed superior therapeutic efficacy on MCF-7 tumor bearing
mice compared to Taxol.
%I ACS Publications