title: Morphology, in vivo distribution and antitumor activity of bexarotene nanocrystals in lung cancer.
abstract: The objective of this study was to develop and evaluate the morphology, biodistribution and antitumor activity of bexarotene nanocrystals delivery system. The morphology was investigated using scanning electron microscopy (SEM), transmission electron microscopy (TEM), atomic force microscope and bexarotene nanocrystals exhibited the advantages of making the efficacy more steady and durable compared with control group in lung with less cardiac accumulation as shown by biodistribution studies in vivo. In addition, MTT assay, flow cytometry analysis, observation of morphological changes and apoptotic body demonstrated that bexarotene nanocrystals could significantly enhance the in vitro cytotoxicity and induced G1 cycle arrest and apoptosis against A549 cells. Also, bexarotene nanocrystals had significant antitumor activity in mice bearing A549 cell line. This finding was correlated with both in vitro and in vivo. Thereby, the overall results suggest that the bexarotene nanocrystals represent a potential source of medicine, which made bexarotene nanocrystals a promising candidate for the treatment of lung cancer.
authors: b Department of Pharmaceutics , School of Pharmaceutical Sciences, Shandong University , Jinan , 250012 , P.R. China.
authors: Yongjie
authors: Y
authors: Wang
authors: a Department of Pharmaceutics , School of Pharmaceutical Sciences, Liaoning University , Shenyang , 110036 , P.R. China.
authors: Jinghong
authors: J
authors: Rong
authors: c Department of Natural Products Chemistry, Key Lab of Chemical Biology (MOE) , School of Pharmaceutical Sciences, Shandong University , Jinan , 250012 , P.R. China.
authors: Jiaozhen
authors: J
authors: Zhang
authors: a Department of Pharmaceutics , School of Pharmaceutical Sciences, Liaoning University , Shenyang , 110036 , P.R. China.
authors: Yu
authors: Y
authors: Liu
authors: a Department of Pharmaceutics , School of Pharmaceutical Sciences, Liaoning University , Shenyang , 110036 , P.R. China.
authors: Xuelian
authors: X
authors: Meng
authors: b Department of Pharmaceutics , School of Pharmaceutical Sciences, Shandong University , Jinan , 250012 , P.R. China.
authors: Hejian
authors: H
authors: Guo
authors: d Research Center for Computer Simulating and Information Processing of Bio-macromolecules of Liaoning Province , Shenyang , 110036 , P.R. China.
authors: Hongsheng
authors: H
authors: Liu
authors: a Department of Pharmaceutics , School of Pharmaceutical Sciences, Liaoning University , Shenyang , 110036 , P.R. China.|d Research Center for Computer Simulating and Information Processing of Bio-macromolecules of Liaoning Province , Shenyang , 110036 , P.R. China.
authors: Lijiang
authors: L
authors: Chen
mesh_terms: D000818:Animals; D016588:Anticarcinogenic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D000077610:Bexarotene; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems / Q000379:methods; D005260:Female; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000378:metabolism* / Q000473:pathology; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D011897:Random Allocation; D013764:Tetrahydronaphthalenes / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D014018:Tissue Distribution / Q000187:drug effects / Q000502:physiology; D047368:Tumor Burden / Q000187:drug effects* / Q000502:physiology
chemical_list: D016588:Anticarcinogenic Agents; D013764:Tetrahydronaphthalenes; D000077610:Bexarotene
keywords: Bexarotene; antitumor activity; characterizations; nanocrystals; tissue distribution