title: Development of lipid nanoparticles for a histone deacetylases inhibitor as a promising anticancer therapeutic.
abstract: BACKGROUND
  Vorinostat (VRS), a histone deacetylases inhibitor, has significant cytotoxic potential in a large number of human cancer cell lines.
  
  
  OBJECTIVE
  To clarify its promising anticancer potential and to improve its drawback related to physical properties and in vivo performance of VRS.
  
  
  METHODS
  VRS was successfully incorporated into nanostructured lipid carriers (NLCs) by the hot microemulsion method using sonication following a homogenization technique.
  
  
  RESULTS
  After the optimization process, VRS-loaded NLCs (VRS-NLCs) were obtained as ideal quality nanoparticles with a spherical shape, small size (∼150 nm), negative charge (∼-22 mV), and narrow size distribution. In addition, the high entrapment efficiency (∼99%) and sustained drug release profile were recorded. Cytotoxicity study in three different cell lines (A549, MCF-7, and SCC-7) demonstrated higher cytotoxicity of VRS-NLCs than free drug. Finally, the AUC of VRS (118.16 ± 17.35 µgh/mL) was enhanced ∼4.4 times compared with that of free drug (27.03 ± 3.25 µgh/mL).
  
  
  CONCLUSIONS
  These results suggest the potential of NLCs as an oral delivery system for enhancement of cellular uptake, in vitro cytotoxicity in cancer cell lines and the oral bioavailability of VRS.
authors.affiliation: a College of Pharmacy , Yeungnam University , Dae-Dong, Gyeongsan , South Korea and.
authors.forename: Tuan Hiep
authors.initials: TH
authors.lastname: Tran
authors.affiliation: b Bio-medicine Pharmacy Applied Research Center , Vietnam Military Medical University , Hanoi , Vietnam.
authors.forename: Duc Thanh
authors.initials: DT
authors.lastname: Chu
authors.affiliation: a College of Pharmacy , Yeungnam University , Dae-Dong, Gyeongsan , South Korea and.
authors.forename: Duy Hieu
authors.initials: DH
authors.lastname: Truong
authors.affiliation: a College of Pharmacy , Yeungnam University , Dae-Dong, Gyeongsan , South Korea and.
authors.forename: Jin Wook
authors.initials: JW
authors.lastname: Tak
authors.affiliation: a College of Pharmacy , Yeungnam University , Dae-Dong, Gyeongsan , South Korea and.
authors.forename: Jee-Heon
authors.initials: JH
authors.lastname: Jeong
authors.affiliation: b Bio-medicine Pharmacy Applied Research Center , Vietnam Military Medical University , Hanoi , Vietnam.
authors.forename: Van Luong
authors.initials: VL
authors.lastname: Hoang
authors.affiliation: a College of Pharmacy , Yeungnam University , Dae-Dong, Gyeongsan , South Korea and.
authors.forename: Chul Soon
authors.initials: CS
authors.lastname: Yong
authors.affiliation: a College of Pharmacy , Yeungnam University , Dae-Dong, Gyeongsan , South Korea and.
authors.forename: Jong Oh
authors.initials: JO
authors.lastname: Kim
mesh_terms: D002152:Calorimetry, Differential Scanning; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D056572:Histone Deacetylase Inhibitors / Q000737:chemistry*; D006801:Humans; D006877:Hydroxamic Acids / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D008055:Lipids / Q000008:administration & dosage* / Q000737:chemistry; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry*; D000077337:Vorinostat
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D056572:Histone Deacetylase Inhibitors; D006877:Hydroxamic Acids; D008055:Lipids; D000077337:Vorinostat
keywords: Histone deacetylases inhibitor; nanostructured lipid carriers; oral bioavailability; vorinostat