title: Formulation, characterization, and geno/cytotoxicity studies of galbanic acid-loaded solid lipid nanoparticles.
abstract: BACKGROUND
  Galbanic acid (GBA) is a sesquiterpene coumarin with different medicinal properties and anticancer effects.
  
  
  OBJECTIVE
  To improve the anticancer activities of GBA, in the current study, we aimed to fabricate GBA-loaded solid lipid nanoparticles (GBA-SLNs) and study their biological activities in vitro.
  
  
  METHODS
  Hot homogenization was used for preparation of GBA-SLNs. The encapsulation efficiency (EE) and drug loading (DL) and in vitro release were determined. MTT, DAPI, DNA fragmentation, comet, and Anexin V apoptosis assays were used to compare the anti-cell proliferation and genotoxicity properties of GBA and GBA-SLNs against A549 cells and HUVEC to detect apoptosis and DNA damage in the final concentration of 100 µM after 48 h treatment.
  
  
  RESULTS
  Scanning electron microscopy (SEM) and particle size analysis showed spherical SLNs (92 nm), monodispersed distribution, and zeta potential of -23.39 mV. High EE (>98%) and long-term in vitro release were achieved. The stability of GBA-SLNs in aqueous medium was approved after 3 months in terms of size and polydispersity index. GBA was able to inhibit A549 growth with an IC50 value of 62 µM at 48 h. Although GBA-SLNs could also inhibit the growth rate of A549 cells, the effect is perceived after 48 h, as approved by the quantitative expression of Bcl-xL and Casp 9 genes, and also genotoxicity assays.
  
  
  CONCLUSIONS
  Long-term apoptotic effect of GBA-SLNs compared with GBA may be due to the accumulation of GBA-SLNs in the tumor site because of deviant tumor pathology. Our data confirmed that SLNs could be exploited for sustained lipophilic GBA delivery.
authors: Research Center for Pharmaceutical Nanotechnology, Tabriz University of Medical Sciences , Tabriz , Iran .
authors: Morteza
authors: M
authors: Eskandani
authors: Jaleh
authors: J
authors: Barar
authors: Jafar Ezzati Nazhad
authors: JE
authors: Dolatabadi
authors: Hamed
authors: H
authors: Hamishehkar
authors: Hossein
authors: H
authors: Nazemiyeh
mesh_terms: D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003374:Coumarins / Q000737:chemistry / Q000494:pharmacology*; D003603:Cytotoxins / Q000494:pharmacology*; D004249:DNA Damage / Q000187:drug effects* / Q000502:physiology; D004305:Dose-Response Relationship, Drug; D061307:Human Umbilical Vein Endothelial Cells; D006801:Humans; D008055:Lipids; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D003374:Coumarins; D003603:Cytotoxins; D008055:Lipids; C048972:galbanic acid
keywords: Anticancer; Ferula ovina; galbanic acid; sesquiterpene coumarin; sustained drug delivery