title: TPGS-modified liposomes for the delivery of ginsenoside compound K against non-small cell lung cancer: formulation design and its evaluation in vitro and in vivo.
abstract: OBJECTIVE
  This work aimed at preparing ginsenoside compound K (GCK)-loaded liposomes modified with TPGS (GCKT-liposomes) to enhance solubility and targeting capability of GCK, as well as inhibit the efflux of GCK from tumour cells.
  
  
  METHODS
  GCKT-liposomes were prepared by the thin-film hydration method and characterized by particle size, polydispersity, zeta potential and drug encapsulation efficiency. A549 cells were used as antitumour cell model to access the cellular uptake of the GCK and perform its antitumour function. The enhancement of in vivo antitumour efficacy of GCKT-liposomes was evaluated by nude mice bearing tumour model.
  
  
  RESULTS
  The results showed that GCKT-liposomes achieved a comparatively high drug loading efficiency and reasonable particle size at the ratio of 7 : 3 (phospholipid: TPGS). The in vitro release demonstrated that the dissolution of GCK was remarkably improved by entrapping it into liposomes. In addition, GCKT-liposomes exhibited a great hypersensitizing effect on A549 cells, and the cellular uptake was enhanced. Compared with free GCK, the IC50 of GCKT-liposomes was significantly reduced (16.3 ± 0.8 vs 24.9 ± 1.0 μg/ml). In vivo antitumour assay also indicated that GCKT-liposomes achieved higher antitumour efficacy (67.5 ± 0.5 vs 40.8 ± 0.7%).
  
  
  CONCLUSIONS
  The novel GCKT-liposomes significantly improved the antitumour efficacy of GCK.
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, China.|College of Pharmacy, Jiangsu University, Zhenjiang, Jiangsu, China.
authors.forename: Lei
authors.initials: L
authors.lastname: Yang
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, China.
authors.forename: Jin
authors.initials: J
authors.lastname: Xin
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, China.
authors.forename: Zhenhai
authors.initials: Z
authors.lastname: Zhang
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, China.
authors.forename: Hongmei
authors.initials: H
authors.lastname: Yan
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Wang
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, China.
authors.forename: E
authors.initials: E
authors.lastname: Sun
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, China.|College of Pharmacy, Jiangsu University, Zhenjiang, Jiangsu, China.
authors.forename: Jian
authors.initials: J
authors.lastname: Hou
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, China.|College of Pharmacy, Jiangsu University, Zhenjiang, Jiangsu, China.
authors.forename: Xiaobin
authors.initials: X
authors.lastname: Jia
authors.affiliation: Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu, China.
authors.forename: Huixia
authors.initials: H
authors.lastname: Lv
mesh_terms: D000072283:A549 Cells; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000627:therapeutic use; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy; D004337:Drug Carriers; D036145:Ginsenosides / Q000008:administration & dosage* / Q000627:therapeutic use; D008081:Liposomes; D008297:Male; D008819:Mice, Nude; D005894:Panax / Q000737:chemistry*; D010743:Phospholipids; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage* / Q000627:therapeutic use; D011092:Polyethylene Glycols; D014810:Vitamin E
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D036145:Ginsenosides; D008081:Liposomes; D010743:Phospholipids; D010936:Plant Extracts; D011092:Polyethylene Glycols; D014810:Vitamin E; C112772:ginsenoside compound K; C014225:tocophersolan
keywords: TPGS; antitumour; ginsenoside compound K; liposomes; non-small cell lung cancer