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Amphiphilic dendrimer engineered nanocarrier systems for co-delivery of siRNA and paclitaxel to matrix metalloproteinase-rich tumors for synergistic therapy

Author：Xin Li, A-ning Sun, Yu-jie Liu, Wen-jie Zhang, Ning Pang, Shi-xuan Cheng & Xian-rong Qi   《NPG asia materials》

ABSTRACTS
Combinations of chemotherapeutics with small interfering RNA (siRNA) can incorporate the advantages of their different mechanisms to exert a synergetic effect. A safe and effective vehicle for simultaneous delivery of the components to tumor cells is a prerequisite for obtaining the optimum effect. We developed an amphiphilic dendrimer engineered nanocarrier system (ADENS) for co-delivering paclitaxel and siRNA for cancer treatment. This nanocarrier possesses a unique hollow core/shell structure in which siRNA is incorporated in the hydrophilic cavity and large quantities of paclitaxel are stored in the hydrophobic interlayer, while the outer PEG layer serves to prolong the circulation time. Further modification by tumor microenvironment-sensitive polypeptides (TMSP) significantly enhanced the cellular uptake, tumor penetration and tumor accumulation of the ADENS by a tumor microenvironment-triggered mechanism. TMSP-ADENS had prominent therapeutic effects at a relatively low drug dose both in vitro and in vivo. In A375 xenograft mice, TMSP-ADENS/siRNA/PTX showed the highest VEGF mRNA inhibition rate of 73% and suppressed tumor growth and relapse, while Taxol did not show an effect on tumor relapse. The anti-tumor and anti-angiogenic effects were further confirmed in an HT-1080 xenograft tumor model. Our findings, combined with the known biodegradability and tunable physicochemical properties of these polymers, suggest that this TMSP-ADENS can be a robust co-delivery system for cancer combination therapy in the future.


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Tumor microenvironment-sensitive peptides ((EGG) 4 -PVGLIG-r 9 -C) and cell penetration peptide (r 9 ) were synthesized via a standard Fmoc solid-phase peptide synthesis method by China Peptides Co., Ltd
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https://www.nature.com/articles/s41427-018-0027-4
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The therapeutic effect of anti-CD52 treatment in murine experimental autoimmune encephalomyelitis is associated with altered IL-33 and ST2 expression levels

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CAS:85466-18-8|Thymopoietin II (32-35)|RKDV

Contact： Liven Qian(钱叶华)-Custom Peptide Mobile: 13761298676（微信） Email：cps037@chinapeptides.net QQ：2880526724 ChinaPeptides Co., Ltd./强耀生物科技有限公司 Name Thymopoietin II (32-35) Code [85466-18-8] The alias Thymopoietin II (32-35) Sequence (single letter abbreviation) RKDV Sequence (three-letter abbreviation) H-Arg-Lys-Asp-Val-OH (trifluoroacetate salt) A basic description TP-4 and TP-3; shortest active thymopoietin II fragments described that exhibit potent immunoregulatory properties in vitro and in vivo. solubility The molecular weight 516.6 Chemical formula C21H40N8O7 The purity 80%，90%，95%，98%，99% Weight 1mg,5mg,10mg,50mg,100mg,1g Storage conditions Store at -20°C. Keep tightly closed. Store in a cool dry place. Number of Residues: 4 1-Letter Code: RKDV 3-Letter Code: Arg-Lys-Asp-Val Molecular weight (Mr): 516.6 g/mol Isoelectric point: 10.1 Net charge at pH 7.0: 1.0 Average hydrophilicity: 1.9 Ratio of hydrophilic residues / total number of residues...
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