title: Novel mucus-penetrating liposomes as a potential oral drug delivery system: preparation, in vitro characterization, and enhanced cellular uptake.
abstract: BACKGROUND
  The aim of this study was to investigate the intestinal mucus-penetrating properties and intestinal cellular uptake of two types of liposomes modified by Pluronic F127 (PF127).
  
  
  METHODS
  The two types of liposomes, ie, PF127-inlaid liposomes and PF127-adsorbed liposomes, were prepared by a thin-film hydration method followed by extrusion, in which coumarin 6 was loaded as a fluorescence marker. A modified Franz diffusion cell mounted with the intestinal mucus of rats was used to study the diffusion characteristics of the two types of PF127 liposomes. Cell uptake studies were conducted in Caco-2 cells and analyzed using confocal laser scanning microcopy as well as flow cytometry.
  
  
  RESULTS
  The diffusion efficiency of the two types of PF127-modified liposomes through intestinal rat mucus was 5-7-fold higher than that of unmodified liposomes. Compared with unmodified liposomes, PF127-inlaid liposomes showed significantly higher cellular uptake of courmarin 6. PF127-adsorbed liposomes showed a lower cellular uptake. Moreover, and interestingly, the two types of PF127-modified liposomes showed different cellular uptake mechanisms in Caco-2 cells.
  
  
  CONCLUSIONS
  PF127-inlaid liposomes with improved intestinal mucus-penetrating ability and enhanced cellular uptake might be a potential carrier candidate for oral drug delivery.
authors.affiliation: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.
authors.forename: Xiuying
authors.initials: X
authors.lastname: Li
authors.forename: Dan
authors.initials: D
authors.lastname: Chen
authors.forename: Chaoyi
authors.initials: C
authors.lastname: Le
authors.forename: Chunliu
authors.initials: C
authors.lastname: Zhu
authors.forename: Yong
authors.initials: Y
authors.lastname: Gan
authors.forename: Lars
authors.initials: L
authors.lastname: Hovgaard
authors.forename: Mingshi
authors.initials: M
authors.lastname: Yang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D018938:Caco-2 Cells; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D007413:Intestinal Mucosa; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D008297:Male; D009093:Mucus / Q000187:drug effects*; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D010539:Permeability; D020442:Poloxamer / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar
chemical_list: D008081:Liposomes; D020442:Poloxamer