title: Rifampicin loaded mannosylated cationic nanostructured lipid carriers for alveolar macrophage-specific delivery.
abstract: OBJECTIVE
  In this study, cationic mannosylated nanostructured lipid carriers (Man-NLCs) were developed for the targeted delivery of rifampicin to alveolar macrophages.
  
  
  METHODS
  Rifampicin loaded Man-NLCs (RFP-Man-NLCs) and rifampicin loaded unmodified nanostructured lipid carriers (REP-NLCs) were prepared using thin film homogenization method and characterized by particle size, polydispersity index, zeta potential, transmission electron microscopy, encapsulation efficiency, pharmacokinetics, biodistribution, cell specific targeting, cytotoxicity and inflammatory response.
  
  
  RESULTS
  RFP-Man-NLCs and REP-NLCs obtained displayed a size distribution around 160 nm (PDI <0.30) with positive charges of approximately 30 mV. The encapsulation efficiency of RFP was above 90%. In the biodistribution study, both RFP-Man-NLCs and RFP-NLCs, compared with the commercially available rifampicin solution, displayed superior lung-targeting ability. Compared to REP-NLCs, RFP-Man-NLCs exhibited significantly higher uptake efficiency in NR8383 cells and alveolar macrophages, which achieved cell-specific targeting. In addition, RFP-Man-NLCs were demonstrated to be a safe formulation with minimum toxicity and no inflammatory response.
  
  
  CONCLUSIONS
  RFP-Man-NLCs provided an alternative strategy for selectively delivering rifampicin to alveolar macrophages.
authors.affiliation: Key Laboratory of Drug Targeting and Drug Delivery Systems, Ministry of Education, Sichuan University, Chengdu, People's Republic of China.
authors.forename: Xu
authors.initials: X
authors.lastname: Song
authors.forename: Qing
authors.initials: Q
authors.lastname: Lin
authors.forename: Ling
authors.initials: L
authors.lastname: Guo
authors.forename: Yao
authors.initials: Y
authors.lastname: Fu
authors.forename: Jianfeng
authors.initials: J
authors.lastname: Han
authors.forename: Huan
authors.initials: H
authors.lastname: Ke
authors.forename: Xun
authors.initials: X
authors.lastname: Sun
authors.forename: Tao
authors.initials: T
authors.lastname: Gong
authors.forename: Zhirong
authors.initials: Z
authors.lastname: Zhang
mesh_terms: D000818:Animals; D000904:Antibiotics, Antitubercular / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002460:Cell Line; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D016676:Macrophages, Alveolar / Q000378:metabolism*; D008297:Male; D008358:Mannose / Q000031:analogs & derivatives; D051379:Mice; D049329:Nanostructures / Q000737:chemistry*; D010316:Particle Size; D017208:Rats, Wistar; D012293:Rifampin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D014018:Tissue Distribution
chemical_list: D000904:Antibiotics, Antitubercular; D004337:Drug Carriers; D008055:Lipids; D008358:Mannose; D012293:Rifampin