title: Enhanced therapeutic efficacy of LHRHa-targeted brucea javanica oil liposomes for ovarian cancer.
abstract: Although brucea javanica oil liposomes (BJOLs) have been used clinically to treat ovarian cancer, its clinical efficacy is often limited by systemic side effects due to non-specific distribution. Luteinizing hormone releasing hormone receptor (LHRHR) is overexpressed in most ovarian cancers but negligibly expressed in most of the other visceral organs. In this study, we aimed to develop a novel LHRHa targeted and BJO-loaded liposomes (LHRHa-BJOLs), and investigate its characteristics, targeting ability and anti-ovarian cancer efficiency both in vitro and in vivo.
  
  
  
  The LHRHa-BJOLs were prepared by film-dispersion and biotin-streptavidin linkage methods, and characterized in terms of its morphology, particle size, zeta potential, ligand conjugation, encapsulation efficiency and stability. The targeting nature and antitumor effects of the liposomes were evaluated in vitro using cultured human ovarian cancer A2780/DDP cells, and in vivo using ovarian cancer-bearing nude mice.
  
  
  
  The LHRHa-BJOLs were successfully synthesized, with a uniformly spherical shape, appropriate particle size and zeta potential, as well as a high encapsulation efficiency. Compared to non-targeted liposomes and BJO emulsion, the LHRHa-BJOLs could significantly increase specific intracellular uptaking rate, enhance cell inhibitory effect and induce cell apoptosis in A2780/DDP cells in vitro. Meanwhile, LHRHa-BJOLs also had a significantly stronger activity of targeting tumor tissue, inhibiting tumor growth, inducing tumor apoptosis and prolonging survival time in ovarian cancer-bearing mice in vivo.
  
  
  
  Our experiment suggests that LHRHa-BJOLs may be a useful targeted drug for the treatment of ovarian cancer.
authors: Department of Obstetrics and Gynecology, Second Affiliated Hospital of Chongqing Medical University, No. 74 Linjiang Road, Yuzhong district, Chongqing, 400010, China.
authors: Hongxia
authors: H
authors: Ye
authors: Department of Obstetrics and Gynecology, Second Affiliated Hospital of Chongqing Medical University, No. 74 Linjiang Road, Yuzhong district, Chongqing, 400010, China.
authors: Xiaojuan
authors: X
authors: Liu
authors: Department of Obstetrics and Gynecology, Second Affiliated Hospital of Chongqing Medical University, No. 74 Linjiang Road, Yuzhong district, Chongqing, 400010, China.
authors: Jiangchuan
authors: J
authors: Sun
authors: Department of Pharmacy, First Affiliated Hospital of Chongqing Medical University, No. 1 Youyi Road, Yuzhong district, Chongqing, 400010, China.
authors: Shenyin
authors: S
authors: Zhu
authors: Department of Obstetrics and Gynecology, Second Affiliated Hospital of Chongqing Medical University, No. 74 Linjiang Road, Yuzhong district, Chongqing, 400010, China.
authors: Yi
authors: Y
authors: Zhu
authors: Department of Obstetrics and Gynecology, Second Affiliated Hospital of Chongqing Medical University, No. 74 Linjiang Road, Yuzhong district, Chongqing, 400010, China. shfch2005@163.com.
authors: Shufang
authors: S
authors: Chang
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D032269:Brucea / Q000737:chemistry*; D049109:Cell Proliferation / Q000187:drug effects; D016503:Drug Delivery Systems; D005260:Female; D007987:Gonadotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D006801:Humans; D008081:Liposomes / Q000008:administration & dosage* / Q000737:chemistry; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D010051:Ovarian Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D010938:Plant Oils / Q000494:pharmacology*; D014407:Tumor Cells, Cultured; D023041:Xenograft Model Antitumor Assays
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D008081:Liposomes; D010938:Plant Oils; D007987:Gonadotropin-Releasing Hormone
keywords: Brucea javanica oil; Liposomes; Luteinizing hormone releasing hormone; Ovarian cancer; Targeted