title: Using rifapentine - hen egg lipoprotein conjugate as macrophage-targeted drug delivery carrier against intracellular Staphylococcus aureus.
abstract: BACKGROUND
  Hen egg low-density lipoprotein (heLDL), which is present in large quantities in egg yolk, share a high identity with human apolipoprotein B-100 precursor.
  
  
  OBJECTIVE
  This study investigated the use of heLDL as a macrophage-targeted drug delivery carrier against intracellular Staphylococcus aureus.
  
  
  METHODS
  Rifapentine (RPT) was incorporated into heLDL (RPT-heLDL). Staphylococcus aureus ATCC 29740 and human U937 macrophage were used as intracellular infection models.
  
  
  CONCLUSIONS
  The loading efficiency of RPT into the heLDL was 66.10 ± 2.28 μg RPT/mg heLDL. Fluorescence microscopy and oil red O staining results indicated RPT-heLDL can be taken up by U937 macrophages. The cell viability (MTT assay) was increased when the concentration of heLDL was <150 μg/mL. Unloaded heLDL (100 μg/mL) can inhibit the growth of intracellular S. aureus compared with the untreated control group after 18 h incubation. RPT-heLDL (6.6 μg/mL RPT, 100 μg/mL heLDL) eliminated 94% of intracellular S. aureus, whereas the corresponding dose of free RPT (6.6 μg/mL) induced an 87% reduction. The in vitro results of the current study indicated that heLDL might be used as a suitable drug carrier for targeting human macrophages.
authors.affiliation: Animal Science Department .
authors.forename: Jinli
authors.initials: J
authors.lastname: Yang
authors.forename: Yuxin
authors.initials: Y
authors.lastname: Li
authors.forename: En
authors.initials: E
authors.lastname: Liu
authors.forename: Tang W
authors.initials: TW
authors.lastname: Xininigen
authors.forename: Wencheng
authors.initials: W
authors.lastname: Bai
authors.forename: Runlin
authors.initials: R
authors.lastname: Han
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002645:Chickens; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D004527:Egg Proteins / Q000737:chemistry; D004530:Egg Yolk / Q000737:chemistry; D006801:Humans; D008074:Lipoproteins / Q000737:chemistry*; D008264:Macrophages / Q000378:metabolism; D008856:Microscopy, Fluorescence; D012293:Rifampin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects*
chemical_list: D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D004527:Egg Proteins; D008074:Lipoproteins; D012293:Rifampin; C018421:rifapentine
keywords: Cytotoxicity; Staphylococcus aureus; hen egg low-density lipoprotein; intracellular bactericidal activities; macrophage drug targeting