title: Pirfenidone-loaded liposomes for lung targeting: preparation and in vitro/in vivo evaluation.
abstract: BACKGROUND
  The purpose of this study was to develop novel pirfenidone (PFD)-loaded liposomes for targeting to the lung.
  
  
  METHODS
  The liposomes were prepared by the film hydration method, and their in vitro/vivo characteristics were evaluated.
  
  
  RESULTS
  The PFD liposomes appeared visually as green to yellowish suspensions and were spherical in shape. The particle size was 582.3±21.6 nm and the entrapment efficiency was relatively high (87.2%±5.7%). The liposomes showed typical sustained and prolonged drug-release behavior in vitro and fitted well with the Weibull distribution equation. The relatively slower time taken to reach a minimal plasma PFD concentration in vivo suggests that PFD liposomes have a sustained-release profile, which is consistent with the results of the in vitro release study. The PFD liposomes showed the largest area under the curve for the lung. The high distribution of PFD achieved in the lungs using this liposomal formulation may be explained by physical entrapment of the liposomes in the vascular network of the lung. Histopathological results indicated that liposomal PFD could alleviate pathological injury in lung tissue.
  
  
  CONCLUSIONS
  This liposomal formulation can enable sustained release of PFD and increase targeting to the lung.
authors.affiliation: Department of Pharmaceuticals, 85th People's Liberation Army Hospital, Shanghai, People's Republic of China.
authors.forename: Hui
authors.initials: H
authors.lastname: Meng
authors.affiliation: Department of Pharmaceuticals, 85th People's Liberation Army Hospital, Shanghai, People's Republic of China.
authors.forename: Yong
authors.initials: Y
authors.lastname: Xu
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D065546:Drug Liberation; D008081:Liposomes; D008168:Lung / Q000378:metabolism*; D051379:Mice; D010316:Particle Size; D011728:Pyridones / Q000008:administration & dosage* / Q000493:pharmacokinetics; D051381:Rats; D014018:Tissue Distribution
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D008081:Liposomes; D011728:Pyridones; C093844:pirfenidone
keywords: histopathological; in vivo; liposomes; lung targeting; pirfenidone