title: Targeted lung cancer therapy using ephrinA1-loaded albumin microspheres.
abstract: OBJECTIVE
  EphrinA1, the ligand of EphA2 receptor tyrosine kinase, has been proven to suppress the growth of tumours. The aim of this study was to conjugate ephrinA1 on the surface of albumin microspheres and investigate the non-small cell lung carcinoma growth and migration in vitro.
  
  
  METHODS
  Bovine serum albumin microspheres were designed and synthesized using a natural polymer albumin by emulsification chemical cross-linking. EphrinA1 was then conjugated on the surface of microspheres by imine formation. The microspheres conjugated with ephrinA1 (ephrinA1-MS) were characterized for particle size, surface morphology, loading efficiency and stability in vitro. The ephrinA1-MS were labelled with fluorescein isothiocyanate to determine phagocytosis. In addition, the effects of ephrinA1-MS on A549 cell growth and migration were determined.
  
  
  RESULTS
  Albumin microspheres exhibited low toxicity for A549 cells (above 90% cell viability). More than 80% of microspheres were phagocytosed within 2 h of incubation. EphrinA1-MS decreased the expression of focal adhesion kinase more effectively than recombinant ephrinA1 alone. Furthermore, ephrinA1-MS showed significant inhibition of non-small cell lung cancer migration when compared with resting cells. EphrinA1-MS attenuated the growth of tumour colonies in matrigels.
  
  
  CONCLUSIONS
  The developed ephrinA1-MS may serve as potential carriers for targeted delivery of the tumour suppressive protein ephrinA1, with minimal cytotoxic effects and greater antitumour therapeutic efficacy against non-small cell lung cancer.
authors: Division of Pulmonary, Critical Care and Sleep Medicine, Department of Medicine, University of Florida, Gainesville, FL 32610, USA.
authors: Hung-Yen
authors: HY
authors: Lee
authors: Kamal A
authors: KA
authors: Mohammed
authors: Shriram
authors: S
authors: Peruvemba
authors: Eugene P
authors: EP
authors: Goldberg
authors: Najmunnisa
authors: N
authors: Nasreen
mesh_terms: D000418:Albumins / Q000737:chemistry; D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000494:pharmacology*; D015153:Blotting, Western; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy*; D002417:Cattle; D045744:Cell Line, Tumor / Q000187:drug effects; D016503:Drug Delivery Systems; D036382:Ephrin-A1 / Q000008:administration & dosage*; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy*; D051379:Mice; D008863:Microspheres; D058990:Molecular Targeted Therapy; D010316:Particle Size
chemical_list: D000418:Albumins; D000964:Antimetabolites, Antineoplastic; D036382:Ephrin-A1