title: Drug delivery with nanospherical supramolecular cell penetrating peptide-taxol conjugates containing a high drug loading.
abstract: OBJECTIVE
  Supramolecular nanostructures via small molecule self-assembly hold great promise for controlled delivery of hydrophobic anticancer drugs. Particularly, taxol has recently been discovered to possess excellent self-assembly property, which may provide new opportunities to develop a new class of functional supramolecular nanomaterials for drug delivery application.
  
  
  METHODS
  A cell penetrating peptide (CPP)-taxol conjugate (Taxol-CPP) was designed and synthesized. The self-assembling property of Taxol-CPP was investigated and the resultant nanomaterials were well characterized. Subsequently, the cytotoxicity of the Taxol-CPP after self-assembly against HepG2 cancer cells was evaluated.
  
  
  RESULTS
  It is found that the Taxol-CPP possesses a high drug loading of 26.4% in each molecule, which is able to self-assemble into supramolecular nanospheres. By taking advantages of the self-assembly ability of taxol, Taxol-CPP supramolecular nanospheres with a mean size of around 130 nm can be obtained, composed of only the functional peptide (CPP) and the drug (taxol). Furthermore, we have demonstrated that the Taxol-CPP nanospheres do not compromise the taxol's potency, which can also be utilized as the carriers for co-delivery of another anticancer drug (doxorubicin).
authors.affiliation: Tianjin Medical University Cancer Institute and Hospital, National Clinical Research Center for Cancer, Key Laboratory of Cancer Prevention and Therapy, Tianjin, Key Laboratory of Breast Cancer Prevention and Therapy, Tianjin Medical University, Ministry of Education, Huan-Hu-Xi Road, Tianjin 300060, PR China.
authors.forename: Ran
authors.initials: R
authors.lastname: Tian
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, Key Laboratory of Bioactive Materials, Ministry of Education, College of Life Sciences, Nankai University, 94 Weijin Road, Tianjin 300071, PR China.
authors.forename: Huaimin
authors.initials: H
authors.lastname: Wang
authors.affiliation: Tianjin Medical University Cancer Institute and Hospital, National Clinical Research Center for Cancer, Key Laboratory of Cancer Prevention and Therapy, Tianjin, Key Laboratory of Breast Cancer Prevention and Therapy, Tianjin Medical University, Ministry of Education, Huan-Hu-Xi Road, Tianjin 300060, PR China. Electronic address: niuruifang@tjmuch.com.
authors.forename: Ruifang
authors.initials: R
authors.lastname: Niu
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, Key Laboratory of Bioactive Materials, Ministry of Education, College of Life Sciences, Nankai University, 94 Weijin Road, Tianjin 300071, PR China. Electronic address: dingd@nankai.edu.cn.
authors.forename: Dan
authors.initials: D
authors.lastname: Ding
mesh_terms: D000595:Amino Acid Sequence; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000494:pharmacology; D057846:Cell-Penetrating Peptides / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D056945:Hep G2 Cells; D006801:Humans; D008969:Molecular Sequence Data; D049329:Nanostructures / Q000737:chemistry* / Q000648:ultrastructure; D009369:Neoplasms / Q000188:drug therapy; D017239:Paclitaxel / Q000008:administration & dosage* / Q000494:pharmacology
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D057846:Cell-Penetrating Peptides; D004337:Drug Carriers; D017239:Paclitaxel
keywords: Cancer therapy; Cell penetrating peptide; Doxorubicin; Drug delivery; Self-assembling peptide; Self-assembly; Supramolecular nanostructures; Taxol