%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