title: Enhanced permeability across Caco-2 cell monolayers by specific mannosylating ligand of buserelin acetate proliposomes.
abstract: BACKGROUND
  Oral delivery of peptide and protein drugs still remains the area of challenges due to their low stability and permeability across GI tract. Among numerous attempts, the receptor-mediated drug targeting is a promising approach to enhance GI permeability.
  
  
  OBJECTIVE
  The aim of this study was to prepare mannosylated buserelin acetate (MANS-BA) proliposome powders grafted with N-octadecyl-d-mannopyranosylamine (SAMAN) as targeting moiety and evaluate their permeability across Caco-2 cell monolayers.
  
  
  METHODS
  The MANS-BA proliposome powders were prepared by coprecipitation method. The targeting moiety SAMAN was synthesized in-house and confirmed by characterization using Fourier transform infrared (FTIR) and differential scanning calorimeter (DSC).
  
  
  RESULTS
  The MANS-BA liposomes reconstituted from proliposome powders exhibited the oligolamellar vesicular structure of phospholipid bilayer. Their size, zeta potential and entrapment efficiency were in the ranges of 93.11-218.95 nm, -24.03 to -37.15 mV and 21.12-33.80%, respectively. The permeability of reconstituted MANS-BA liposomes across Caco-2 cell monolayers was significantly enhanced to about 1.2- and 2.2-fold over those of conventional BA liposomes and solution, respectively.
  
  
  CONCLUSIONS
  Increase in dicetylphosphate, cholesterol and SAMAN contents resulted in significant increase in size and zeta potential of reconstituted MAN-BA liposomes. The entrapment efficiency was increased with increasing dicetylphosphate and mannitol contents in liposomes containing cholesterol.
  
  
  CONCLUSIONS
  The significantly enhanced permeability across Caco-2 cell monolayers of MANS-BA liposomes might be due to the role of mannose receptor on intestinal enterocytes.
authors.affiliation: a Department of Manufacturing Pharmacy, Faculty of Pharmacy , Mahidol University , Bangkok , Thailand .
authors.forename: Koson
authors.initials: K
authors.lastname: Yingsukwattana
authors.affiliation: a Department of Manufacturing Pharmacy, Faculty of Pharmacy , Mahidol University , Bangkok , Thailand .
authors.forename: Satit
authors.initials: S
authors.lastname: Puttipipatkhachorn
authors.affiliation: b National Nanotechnology Center, National Science and Technology Development Agency , Pathumthani , Thailand , and.
authors.forename: Uracha
authors.initials: U
authors.lastname: Ruktanonchai
authors.affiliation: c Division of Pharmaceutical Sciences, Faculty of Pharmacy , Thammasat University, Rangsit Center , Pathumthani , Thailand.
authors.forename: Narong
authors.initials: N
authors.lastname: Sarisuta
mesh_terms: D000606:Amino Sugars / Q000138:chemical synthesis / Q000737:chemistry*; D002064:Buserelin / Q000138:chemical synthesis / Q000737:chemistry*; D018938:Caco-2 Cells; D006801:Humans; D008024:Ligands; D008081:Liposomes / Q000138:chemical synthesis / Q000737:chemistry*; D010539:Permeability
chemical_list: D000606:Amino Sugars; D008024:Ligands; D008081:Liposomes; C575355:N-octadecylmannopyranosylamine; D002064:Buserelin
keywords: Buserelin acetate; Caco-2 cells; nanotechnology; permeation; proliposomes; targeting