Matches in SemOpenAlex for { <https://semopenalex.org/work/W2793669845> ?p ?o ?g. }
- W2793669845 endingPage "473" @default.
- W2793669845 startingPage "466" @default.
- W2793669845 abstract "Background: RX-0201 is an antisense oligonucleotide (ASO) against Akt1 currently in clinical trial for metastatic renal cancer.Purpose: To improve the delivery of RX-0201 using folate receptor-targeted lipid-albumin nanoparticles (F-LAN).Methods: F-LAN were synthesized with the composition of DOTAP/soyPC/TPGS/folate-PEG-DSPE (25:70:4:1 m/m), a cationic human serum albumin-pentaethylenehexamine (HSA-PEHA) conjugate and RX-0201. The nanoparticles were evaluated in KB human carcinoma cells in vitro and in a KB murine xenograft tumour model in vivo for pharmacokinetics and antitumor activities.Results: The F-LAN-RX-0201 had a mean particle size of 108.6 ± 5.8 nm, zeta potential of 10.5 ± 3.2 mV and ASO loading efficiency of 71.5 ± 4.5%. In KB cells, uptake and Akt1 inhibition by F-LAN-RX-0201 were greater than those of non-targeted LAN-RX-0201 and could be partially blocked by excess free folate. F-LAN-RX-0201 inhibited cell growth with an IC50 of 11.9 μM. In contrast, LAN-RX-0201 showed lower cytotoxicity with an IC50 of 32.0 μM. No significant cytotoxicity was observed with up to 250 µM of free RX-0201. Pharmacokinetic studies showed that F-LAN-RX-0201 had a longer terminal half-life than free RX-0201 (442 vs. 219 min). In a KB xenograft tumour model, F-LAN-RX-0201 exhibited greater tumour inhibition than LAN-RX-0201 at 16 mg/kg. Moreover, F-LAN-RX-0201 at 16 mg/kg showed comparable tumour inhibition compared to free RX-0201 at a much higher dose of 90 mg/kg.Conclusions: F-LAN-RX-0201 showed promise as a therapeutic agent for tumours with elevated folate-receptor expression." @default.
- W2793669845 created "2018-03-29" @default.
- W2793669845 creator A5009480635 @default.
- W2793669845 creator A5014068004 @default.
- W2793669845 creator A5022643931 @default.
- W2793669845 creator A5023363049 @default.
- W2793669845 creator A5040022220 @default.
- W2793669845 creator A5043949272 @default.
- W2793669845 creator A5045865635 @default.
- W2793669845 creator A5050738516 @default.
- W2793669845 creator A5080149754 @default.
- W2793669845 creator A5082156756 @default.
- W2793669845 date "2018-02-08" @default.
- W2793669845 modified "2023-10-12" @default.
- W2793669845 title "Folate receptor-targeted lipid-albumin nanoparticles (F-LAN) for therapeutic delivery of an Akt1 antisense oligonucleotide" @default.
- W2793669845 cites W112828355 @default.
- W2793669845 cites W1487234933 @default.
- W2793669845 cites W1981551573 @default.
- W2793669845 cites W1984621921 @default.
- W2793669845 cites W1990421621 @default.
- W2793669845 cites W1995856367 @default.
- W2793669845 cites W2005564022 @default.
- W2793669845 cites W2010680800 @default.
- W2793669845 cites W2027548179 @default.
- W2793669845 cites W2027689392 @default.
- W2793669845 cites W2031469256 @default.
- W2793669845 cites W2035258932 @default.
- W2793669845 cites W2038300196 @default.
- W2793669845 cites W2043361950 @default.
- W2793669845 cites W2060882819 @default.
- W2793669845 cites W2065230239 @default.
- W2793669845 cites W2066588182 @default.
- W2793669845 cites W2075556692 @default.
- W2793669845 cites W2080879368 @default.
- W2793669845 cites W2088318176 @default.
- W2793669845 cites W2096512737 @default.
- W2793669845 cites W2109909805 @default.
- W2793669845 cites W2112911113 @default.
- W2793669845 cites W2127488207 @default.
- W2793669845 cites W2147071344 @default.
- W2793669845 cites W2230291341 @default.
- W2793669845 cites W2339579270 @default.
- W2793669845 cites W2397198015 @default.
- W2793669845 cites W2414174916 @default.
- W2793669845 cites W2557961665 @default.
- W2793669845 cites W26051613 @default.
- W2793669845 doi "https://doi.org/10.1080/1061186x.2018.1433678" @default.
- W2793669845 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29376449" @default.
- W2793669845 hasPublicationYear "2018" @default.
- W2793669845 type Work @default.
- W2793669845 sameAs 2793669845 @default.
- W2793669845 citedByCount "13" @default.
- W2793669845 countsByYear W27936698452018 @default.
- W2793669845 countsByYear W27936698452019 @default.
- W2793669845 countsByYear W27936698452020 @default.
- W2793669845 countsByYear W27936698452021 @default.
- W2793669845 countsByYear W27936698452022 @default.
- W2793669845 countsByYear W27936698452023 @default.
- W2793669845 crossrefType "journal-article" @default.
- W2793669845 hasAuthorship W2793669845A5009480635 @default.
- W2793669845 hasAuthorship W2793669845A5014068004 @default.
- W2793669845 hasAuthorship W2793669845A5022643931 @default.
- W2793669845 hasAuthorship W2793669845A5023363049 @default.
- W2793669845 hasAuthorship W2793669845A5040022220 @default.
- W2793669845 hasAuthorship W2793669845A5043949272 @default.
- W2793669845 hasAuthorship W2793669845A5045865635 @default.
- W2793669845 hasAuthorship W2793669845A5050738516 @default.
- W2793669845 hasAuthorship W2793669845A5080149754 @default.
- W2793669845 hasAuthorship W2793669845A5082156756 @default.
- W2793669845 hasConcept C109316439 @default.
- W2793669845 hasConcept C150903083 @default.
- W2793669845 hasConcept C153911025 @default.
- W2793669845 hasConcept C185592680 @default.
- W2793669845 hasConcept C192562407 @default.
- W2793669845 hasConcept C202751555 @default.
- W2793669845 hasConcept C207001950 @default.
- W2793669845 hasConcept C55493867 @default.
- W2793669845 hasConcept C86803240 @default.
- W2793669845 hasConcept C98274493 @default.
- W2793669845 hasConceptScore W2793669845C109316439 @default.
- W2793669845 hasConceptScore W2793669845C150903083 @default.
- W2793669845 hasConceptScore W2793669845C153911025 @default.
- W2793669845 hasConceptScore W2793669845C185592680 @default.
- W2793669845 hasConceptScore W2793669845C192562407 @default.
- W2793669845 hasConceptScore W2793669845C202751555 @default.
- W2793669845 hasConceptScore W2793669845C207001950 @default.
- W2793669845 hasConceptScore W2793669845C55493867 @default.
- W2793669845 hasConceptScore W2793669845C86803240 @default.
- W2793669845 hasConceptScore W2793669845C98274493 @default.
- W2793669845 hasIssue "5-6" @default.
- W2793669845 hasLocation W27936698451 @default.
- W2793669845 hasLocation W27936698452 @default.
- W2793669845 hasOpenAccess W2793669845 @default.
- W2793669845 hasPrimaryLocation W27936698451 @default.
- W2793669845 hasRelatedWork W1592261125 @default.
- W2793669845 hasRelatedWork W1982027601 @default.
- W2793669845 hasRelatedWork W1983855168 @default.
- W2793669845 hasRelatedWork W200909032 @default.