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Highly efficacious and specific anti-glioma chemotherapy by tandem nanomicelles co-functionalized with brain tumor-targeting and cell-penetrating peptides

文献作者：Yaqin Zhu, Yu Jiang, Fenghua Meng, Chao Deng, Ru Cheng, Jian Zhang, Jan Feijen, Zhiyuan Zhong   《Journal of Controlled Release》

ABSTRACTS
Glioma is a highly challenging human malignancy as drugs typically exhibit a low blood-brain barrier (BBB) permeability as well as poor glioma selectivity and penetration. Here, we report that tandem nanomicelles co-functionalized with brain tumor-targeting and cell-penetrating peptides, Angiopep-2 and TAT, enable a highly efficacious and specific anti-glioma chemotherapy. Interestingly, tandem nanomicelles with 20?mol% Angiopep-2 and 10?mol% TAT linked via long and short poly(ethylene glycol)s, respectively, while maintaining a high glioma cell selectivity display markedly enhanced BBB permeation, glioma accumulation and penetration, and glioma cell uptake. We further show that docetaxel-loaded tandem nanomicelles have a long blood circulation time in mice and significantly better inhibit orthotopic U87MG human glioma than the corresponding Angiopep-2 single peptide-functionalized control, leading to an improved survival rate with little adverse effects. These tandem nanomicelles uniquely combining brain tumor-targeting and cell-penetrating functions provide a novel and effective strategy for targeted glioma therapy.

Graphical abstract


KEY WORDS
Nanomicelles; Reduction-sensitive; Glioma; TAT; Blood-brain barrier.
SCREENSHOT

RELATED PRODUCTS
Angiopep-2 (ANG, 95%, TFFYGGSRGKRNNFKTEEYC) and TAT (98%, YGRKKRRQRRRC) (ChinaPeptides Co., Ltd., Shanghai, China) 
CHAINING
https://www.sciencedirect.com/science/article/pii/S016836591830155X
Number of Residues:20
1-Letter Code:TFFYGGSRGKRNNFKTEEYC
3-Letter Code:Thr-Phe-Phe-Tyr-Gly-Gly-Ser-Arg-Gly-Lys-Arg-Asn-Asn-Phe-Lys-Thr-Glu-Glu-Tyr-Cys

Molecular weight (Mr):2404.65 g/mol
Isoelectric point:9.5
Net charge at pH 7.0:2.0
Average hydrophilicity:0.2
Ratio of hydrophilic residues / total number of residues:45 %

Number of Residues:12
1-Letter Code:YGRKKRRQRRRC
3-Letter Code:Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Cys

Molecular weight (Mr):1662.99 g/mol
Isoelectric point:12.4
Net charge at pH 7.0:8.0
Average hydrophilicity:1.7
Ratio of hydrophilic residues / total number of residues:75 %
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