The limitations of anticancer drugs, including poor tumor targeting and weak uptake
efficiency, are important factors affecting tumor therapy. According to characteristics of
the tumor microenvironment, in this study, we aimed to synthesize matrix metalloproteinase
(MMP)-responsive curcumin (Cur)-loaded nanoparticles (Cur-P-NPs) based on amphiphilic
block copolymer (MePEG-peptide-PET-PCL) with MMP-cleavable peptide (GPLGIAGQ) and
penetrating peptide (r9), modified to improve tumor targeting and cellular uptake. The
average size of Cur-P-NPs was 176.9 nm, with a zeta potential of 8.1 mV, and they showed
drug entrapment efficiency and a loading capacity of 87.07% ± 0.63% and 7.44% ± 0.16%,
respectively. Furthermore, Cur release from Cur-P-NPs was sustained for 144 h at pH 7.4,
and the release rate was accelerated under enzyme reaction condition. The MTT assay
demonstrated that free P-NPs had favorable biosafety, and the anti-proliferative activity
of Cur-P-NPs was positively correlated with Cur concentration in MCF-7 cells.
Additionally, the results of cellular uptake, in vivo pharmacokinetics, and
biodistribution showed that Cur-P-NPs had a good effect on cellular uptake and tumor
targeting, resulting in the best bioavailability in tumor therapy. Therefore, Cur-P-NPs,
as a promising drug delivery system, might lead to a new and efficient route for targeted
therapy in clinical practice.
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