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Targeted osteosarcoma chemotherapy using RGD peptide-installed doxorubicin-loaded biodegradable polymeric micelle

文献作者：Zhenhua Fang, Yanpeng Sun, Hong Xiao, Peng Li, Ming Liu, Fan Ding, Wusheng Kan, Runsheng Miao   《Biomedicine & Pharmacotherapy》

ABSTRACTS
Osteosarcoma is the most common primary malignant bone tumor in the pediatric age group, and chemotherapy directed by targeted nanoparticulate drug delivery system represents a promising approach for osteosarcoma treatment recently. Here, we designed and developed a novel DOX-loaded targeted polymeric micelle self-assembled from RGD-terminated poly(ethylene glycol)-block-poly (trimethylene carbonate) (RGD-PEG-PTMC) amphiphilic biodegradable block copolymer, for high-efficiency targeted chemotherapy of osteosarcoma. Notably, the RGD-installed DOX-loaded biodegradable polymeric micelle (RGD-DOX-PM) with drug loading efficiency of 57%–73% displayed a narrow distribution (PDI = 0.05–0.12) with average sizes ranging from 46 to 73 nm depending on the DOX loading content. The release amount of DOX from RGD-DOX-PM achieved 63% within 60 h under physiological condition. Interestingly, MTT assays in MG-63 and MNNG/HOS osteosarcoma cells exhibited that half-maximal inhibitory concentration (IC50) value of RGD-DOX-PM was much lower than its non-targeted counterpart (DOX-PM), implying RGD decorated nanoparticles had enhanced cell targeting ability and led to more effective anti-tumor effect. Furthermore, the targeting ability of RGD-DOX-PM was confirmed by in vitroflow cytometry and confocal laser scanning microscopy (CLSM) imaging assays, where the results showed more RGD-DOX-PM were taken up by MG-63 cells than that of DOX-PM. Therefore, this RGD decorated DOX-loaded polymeric micelle is promising for targeted chemotherapy of osteosarcoma.
KEY WORDS
Osteosarcoma; Targeted chemotherapy; Nanoparticulate drug delivery system; RGD.
SCREENSHOT

RELATED PRODUCTS
RGD peptide (GCGYGRGDSPG, 98%, China Peptides Co., Ltd.)
CHAINING
https://www.sciencedirect.com/science/article/abs/pii/S0753332216314305
Number of Residues:11
1-Letter Code:GCGYGRGDSPG
3-Letter Code:Gly-Cys-Gly-Tyr-Gly-Arg-Gly-Asp-Ser-Pro-Gly

Molecular weight (Mr):1025.07 g/mol
Isoelectric point:6.2
Net charge at pH 7.0:0.0
Average hydrophilicity:0.3
Ratio of hydrophilic residues / total number of residues:27 %

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