title: Mannosylated lipid nano-emulsions loaded with lycorine-oleic acid ionic complex for tumor cell-specific delivery.
abstract: This study was to prepare a mannosylated lycorine lipid nano-emulsion formulation (M-LYC-OA-LNEs) for the aim of achieving tumor targeting delivery of lycorine (LYC) . The low lipophilicity of LYC made it hard to be dispersed into lipid nano-emulsions (LNEs). In order to increase its lipophilicity, lycorine-oleic acid ionic complex (LYC-OA) was made. M-LYC-OA-LNEs and uncoated lycorine-oleic acid loaded lipid nano-emulsions (LYC-OA-LNEs) were prepared by solvent injection method and characterized by transmission electron microscopy (TEM), particle size, polydispersity index, zeta-potential and entrapment efficiency analysis. The in vitro cellular uptake and growth inhibition activity studies were performed on A549 cell lines. The entrapment efficiency of M-LYC-OA-LNEs was 82.7 ± 1.6 %. The cellular uptake study showed that coated LNEs were preferably taken up by A549 cells than uncoated LNEs. The effective test by MTT assay showed better growth inhibition activity of M-LYC-OA-LNEs on A549 cell lines when compared with LYC-OA-LNEs and blank LNEs. These results demonstrated that M-LYC-OA-LNEs could be a promising formulation for tumor targeting delivery of LYC with the potential of being applied in the diagnosis and treatment of cancer.
authors.affiliation: Key Laboratory of Drug Targeting and Drug Delivery System, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, China.
authors.forename: Yangming
authors.initials: Y
authors.lastname: Guo
authors.forename: Xing
authors.initials: X
authors.lastname: Liu
authors.forename: Xun
authors.initials: X
authors.lastname: Sun
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhang
authors.forename: Tao
authors.initials: T
authors.lastname: Gong
authors.forename: Zhirong
authors.initials: Z
authors.lastname: Zhang
mesh_terms: D047151:Amaryllidaceae Alkaloids / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D016466:CHO Cells; D049109:Cell Proliferation / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D006224:Cricetinae; D003412:Cricetulus; D016503:Drug Delivery Systems; D004655:Emulsions / Q000737:chemistry; D020128:Inhibitory Concentration 50; D042541:Intracellular Space / Q000378:metabolism; D007477:Ions; D008358:Mannose / Q000737:chemistry*; D018613:Microscopy, Confocal; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D009369:Neoplasms / Q000188:drug therapy*; D019301:Oleic Acid / Q000737:chemistry*; D010316:Particle Size; D010617:Phenanthridines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D012995:Solubility; D055672:Static Electricity
chemical_list: D047151:Amaryllidaceae Alkaloids; D004655:Emulsions; D007477:Ions; D010617:Phenanthridines; D019301:Oleic Acid; C015330:lycorine; D008358:Mannose