2014
DOI: 10.1002/ardp.201300415
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Cell‐Penetrable Lysine Dendrimers for Anti‐Cancer Drug Delivery: Synthesis and Preliminary Biological Evaluation

Abstract: Improving the cell penetration and enhancing the cell selectivity of drugs have been approved for overcoming the major drawbacks of chemotherapeutic agents: the toxicity to normal cells and the drug resistance in tumors. In this paper, lysine dendrimers (G1-G3) were chosen as novel cell-penetrating carriers for anti-cancer drugs based on the internalization mechanism of cell-penetrating peptides and the characteristics of dendritic peptides. After labeling with fluorescein isothiocyanate (FITC), the cell-penet… Show more

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Cited by 16 publications
(10 citation statements)
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References 36 publications
(37 reference statements)
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“…Moreover, it is widely accepted that nanoparticles can be easily absorbed by cells (Thurn et al 2011;Sokolova et al 2013). For this reason, a variety of nanoparticle systems are currently being explored for cancer therapeutics (Haley and Frenkel 2008), which include dendrimers (Zhao et al 2014), liposome (Allison 2007;Bovis et al 2012), micelles (Lee et al 2003), carbon nanotubes (Huang et al 2010), and polymeric nanoparticles (Kumari et al 2010;Li and Liu 2014). Several nanoparticles based on organic and inorganic chromophores, which show strong absorption in the near-infrared (NIR) tissuetransparency window, such as gold and carbon nanomaterials, have displayed encouraging photothermal therapeutic efficacy in preclinical animal experiments (Yuan et al 2012;Chu et al 2013).…”
Section: Introductionmentioning
confidence: 99%
“…Moreover, it is widely accepted that nanoparticles can be easily absorbed by cells (Thurn et al 2011;Sokolova et al 2013). For this reason, a variety of nanoparticle systems are currently being explored for cancer therapeutics (Haley and Frenkel 2008), which include dendrimers (Zhao et al 2014), liposome (Allison 2007;Bovis et al 2012), micelles (Lee et al 2003), carbon nanotubes (Huang et al 2010), and polymeric nanoparticles (Kumari et al 2010;Li and Liu 2014). Several nanoparticles based on organic and inorganic chromophores, which show strong absorption in the near-infrared (NIR) tissuetransparency window, such as gold and carbon nanomaterials, have displayed encouraging photothermal therapeutic efficacy in preclinical animal experiments (Yuan et al 2012;Chu et al 2013).…”
Section: Introductionmentioning
confidence: 99%
“…Moreover, it decreases toxic effects to normal tissues and the pHsensitive bond is fast cleaved in acidic conditions. 43 Based on the use of CPP-dendrimer derived (CPPD) for increasing the internalization of drugs, 44,45 Zhao et al 44 (2014) investigated the cell penetrable lysine dendrimers conjugate with 5-fluororacil (G1-G3). The authors observed some advantages such as stability, low toxicity to normal cells, although moderate activity in tumors was demonstrated.…”
Section: R a F Tmentioning
confidence: 99%
“…Similarly, Mcguigan et al have disclosed NUC-1031, a gemcitabine phosphoramidate prodrug that has shown significant reduction in viability of tumor cells [187]. Zhao et al demonstrated the efficacy of cell penetrable dendrimer as a potential antitumor drug carrier by 5-FU and lysine dendrimer conjugates [188]. Several nanocarriers like PEGylated lipids for squalenoyl amphiphilic prodrugs of gemcitabine and dideoxycytidine [189] and polymeric micelles for stearoyl-gemcitabine [190] are being developed to improve the efficacy and sustainability of the anticancer properties.…”
Section: Prodrug Approach: Analog / Chemical Conjugation For Cancementioning
confidence: 99%