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Nian-Qiu Shi,1 Yan Li,2 Yong Zhang,3 Zheng-Qiang Li,4 Xian-Rong Qi5 1School of Pharmacy, Jilin Medical University, Jilin, Jilin, 132013, China; 2Immunology Department, Laboratory Medical College, Jilin Medical University, Jilin, Jilin, 132013, China; 3College of Life Science, Jilin University, Changchun, Jilin, 130012, China; 4Key Laboratory for Molecular Enzymology and Engineering, Ministry of Education, College of Life Science, Jilin University, Changchun, Jilin, 130012, China; 5Department of Pharmaceutics, School of Pharmaceutical Science, Peking University, Beijing, 100191, China Introduction: Acceleration and improvement of penetration across cell-membrane interfaces of active targeted nanotherapeutics into tumor cells would improve tumor-therapy efficacy by overcoming the issue of poor drug penetration. Cell-penetrating peptides, especially synthetic polyarginine, have shown promise in facilitating cargo delivery. However, it is unknown whether polyarginine can work to overcome the membrane interface in an inserted pattern for cyclic peptide ligand-mediated active targeting drug delivery. Here, we conducted a study to test the hypothesis that tandem-insert nona-arginine (tiR9) can act as an accelerating component for intracellular internalization, enhance cellular penetration, and promote antitumor efficacy of active targeted cyclic asparagine–glycine–arginine (cNGR)-decorated nanoliposomes. Methods: Polyarginine was coupled with the polyethylene glycol (PEG) chain and the cNGR moiety, yielding a cNGR–tiR9–PEG2,000–distearoylphosphatidylethanolamine conjugate. Results: The accelerating active targeted liposome (Lip) nanocarrier (cNGR-tiR9-Lip–doxorubicin [Dox]) constructed in this study held suitable physiochemical features, such as appropriate particle size of ~150 nm and sustained-release profiles. Subsequently, tiR9 was shown to enhance cellular drug delivery of Dox-loaded active targeted systems (

Nian-Qiu Shi,1 Yan Li,2 Yong Zhang,3 Zheng-Qiang Li,4 Xian-Rong Qi5 1School of Pharmacy, Jilin Medical University, Jilin, Jilin, 132013, China; 2Immunology Department, Laboratory Medical College, Jilin Medical University, Jilin, Jilin, 132013, China; 3College of Life Science, Jilin University, Changchun, Jilin, 130012, China; 4Key Laboratory for Molecular Enzymology and Engineering, Ministry of Education, College of Life Science, Jilin University, Changchun, Jilin, 130012, China; 5Department of Pharmaceutics, School of Pharmaceutical Science, Peking University, Beijing, 100191, China Introduction: Acceleration and improvement of penetration across cell-membrane interfaces of active targeted nanotherapeutics into tumor cells would improve tumor-therapy efficacy by overcoming the issue of poor drug penetration. Cell-penetrating peptides, especially synthetic polyarginine, have shown promise in facilitating cargo delivery. However, it is unknown whether polyarginine can work to overcome the membrane interface in an inserted pattern for cyclic peptide ligand-mediated active targeting drug delivery. Here, we conducted a study to test the hypothesis that tandem-insert nona-arginine (tiR9) can act as an accelerating component for intracellular internalization, enhance cellular penetration, and promote antitumor efficacy of active targeted cyclic asparagine–glycine–arginine (cNGR)-decorated nanoliposomes. Methods: Polyarginine was coupled with the polyethylene glycol (PEG) chain and the cNGR moiety, yielding a cNGR–tiR9–PEG2,000–distearoylphosphatidylethanolamine conjugate. Results: The accelerating active targeted liposome (Lip) nanocarrier (cNGR-tiR9-Lip–doxorubicin [Dox]) constructed in this study held suitable physiochemical features, such as appropriate particle size of ~150 nm and sustained-release profiles. Subsequently, tiR9 was shown to enhance cellular drug delivery of Dox-loaded active targeted systems (