| Chiu SJ |
------>authors3_c= ------>paper_class1=1 ------>Impact_Factor=1.390 ------>paper_class3=2 ------>paper_class2=1 ------>vol=26 ------>confirm_bywho=None ------>insert_bywho=sjchiu ------>Jurnal_Rank=84.4 ------>authors4_c= ------>comm_author= ------>patent_EDate=None ------>authors5_c= ------>publish_day=1 ------>paper_class2Letter=None ------>page2=1056 ------>medlineContent= ------>unit=000 ------>insert_date=20060501 ------>iam=1 ------>update_date=None ------>author=??? ------>change_event=2 ------>ISSN=0250-7005 ------>authors_c=??? ------>score=500 ------>journal_name=Anticancer Research ------>paper_name=Efficient delivery of an antisense oligodeoxyribonucleotide formulated in folate receptor-targeted liposomes ------>confirm_date=None ------>tch_id=094123 ------>pmid=16619505 ------>page1=1049 ------>fullAbstract=BACKGROUND: Folate receptors (FRs) are cellular surface markers for numerous solid tumors and myeloid leukemias. The aim of this study was to develop an antisense oligodeoxyribonucleotide (ODN) carrier targeting FR-overexpressing cancer cells using folate (FA) as the targeting moiety. G3139, a phosphorothioate antisense ODN against human bcl2 mRNA, was evaluated in this study. MATERIALS AND METHODS: G3139-containing liposomes were prepared using an ethanol dilution method. For the targeted formulation, 0.5 mol% of folate-PEG-DSPE was incorporated as a targeting ligand into cationic liposomes composed of DC-Chol/egg PC/PEG-DSPE at 25:65:10 mol/mol. Particle size and surface charge were measured and cellular uptake was assessed by fluorescence microscopy and flow cytometry. The ODN-containing formulations were evaluated in FR+ KB cells for Bcl2 down-regulation measured by Western blot. The cytotoxicity of the formulations was determined by MTT assay. RESULTS: The G3139-containing liposomes had an average diameter of 80-90 nm with high ODN entrapment efficiency (70-80%). Incorporation of the folate ligand did not significantly alter the particle size and entrapment efficiency. The formulation exhibited colloidal stability in a serum-containing environment. In uptake studies, the folate-targeted formulation showed ligand concentration-dependent uptake that was up to 6-fold more efficient than that of the non-targeted formulation (p < 0.05). The uptake could be blocked by an excess amount of free folate, thus indicating an FR-dependent mechanism. CONCLUSION: FR-targeted G3139-containing liposomes showed promising transfection activity in KB cells. FR-targeted formulations were capable of specific targeting to FR-overexpressing cell lines and optimizing the amount of folate ligand in the liposomal formulation can result in more efficient antisense delivery. ------>tmu_sno=None ------>sno=13533 ------>authors2=Marcucci G ------>authors3=Lee RJ ------>authors4= ------>authors5= ------>authors6= ------>authors6_c= ------>authors=Chiu SJ ------>delete_flag=0 ------>SCI_JNo=None ------>authors2_c= ------>publish_area=0 ------>updateTitle=Efficient delivery of an antisense oligodeoxyribonucleotide formulated in folate receptor-targeted liposomes. ------>language=2 ------>check_flag=None ------>submit_date=None ------>country=None ------>no=2A ------>patent_SDate=None ------>update_bywho=None ------>publish_year=2006 ------>submit_flag=None ------>publish_month=4 |