title: Tyroservatide-TPGS-paclitaxel liposomes: Tyroservatide as a targeting ligand for improving breast cancer treatment.
abstract: Tyroservatide (YSV) is a tripeptide that has been approved for clinical testing, as a new anticancer drug. In the current study, YSV-stearic acid (YSV-SA) was inserted into the surface of d-alpha-tocopheryl polyethylene glycol 1000 succinate monoester (TPGS)-modified paclitaxel (PTX) liposomes (TP-Lip) to form YSV-conjugated TP-Lip (TYP-Lip). Both in vivo imaging and in vitro cell uptake analysis indicated that these modifications could increase tumor-targeting and cell uptake of the liposomes. Optimal antitumor effects were achieved via tail vein injections of TYP-Lip in MB-231 tumor-bearing nude mice. Overall, the formed TYP-Lip not only achieved a synergistic anticancer effect through YSV and PTX, but also improved tumor-targeting and exhibited further antitumor capabilities. These results indicated that combining biological (YSV) and chemotherapeutic (PTX) agents is an efficient combinatorial delivery strategy for enhanced tumor targeting and synergistic antitumor effects.
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, China; Department of Hospital Pharmacy, The First Hospital of Suqian, Suqian, China.
authors.forename: Xin
authors.initials: X
authors.lastname: Jin
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, China.
authors.forename: Mengying
authors.initials: M
authors.lastname: Li
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, China.
authors.forename: Lifang
authors.initials: L
authors.lastname: Yin
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, China.
authors.forename: Jianping
authors.initials: J
authors.lastname: Zhou
authors.affiliation: Jiangsu Province Hospital on Integration of Chinese and Western Medicine affiliated with Nanjing University of Chinese Medicine, Nanjing, China. Electronic address: davidpharm@yeah.net.
authors.forename: Zhenhai
authors.initials: Z
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, China. Electronic address: lvhuixia@163.com.
authors.forename: Huixia
authors.initials: H
authors.lastname: Lv
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D000971:Antineoplastic Combined Chemotherapy Protocols / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use; D001940:Breast / Q000187:drug effects* / Q000473:pathology; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D004338:Drug Combinations; D016503:Drug Delivery Systems; D005260:Female; D006801:Humans; D008081:Liposomes / Q000737:chemistry*; D051379:Mice; D008819:Mice, Nude; D009842:Oligopeptides / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D017239:Paclitaxel / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D014810:Vitamin E / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D004338:Drug Combinations; D008081:Liposomes; D009842:Oligopeptides; C510683:tripeptide tyroservatide; D014810:Vitamin E; C014225:tocophersolan; D017239:Paclitaxel
keywords: Co-delivery; Paclitaxel; Synergy effect; Tumor targeting; Tyroservatide