PMID- 20014431
OWN - NLM
STAT- MEDLINE
DCOM- 20100625
LR  - 20121115
IS  - 1520-6017 (Electronic)
IS  - 0022-3549 (Linking)
VI  - 99
IP  - 5
DP  - 2010 May
TI  - Impact of membrane properties on uptake and transcytosis of colloidal 
      nanocarriers across an epithelial cell barrier model.
PG  - 2423-33
LID - 10.1002/jps.22001 [doi]
AB  - The aim of this study was to investigate the effect of liposomal membrane 
      properties on cellular uptake and transcytosis across a tight Madin-Darby canine 
      kidney (MDCK) cell barrier in vitro. More than 25 small vesicles were prepared by 
      lipid film hydration/extrusion to generate small unilamellar vesicles. The 
      fluorescence marker calcein was encapsulated to mimic hydrophilic drug transport. 
      Marker uptake by MDCK cells seems to be mediated by different mechanisms for the 
      liposomes used. It was mainly depending on membrane fluidity and vesicle charge. 
      Liposomes L2 with a positive charge (325 +/- 3 pmol/well) and vesicles L3 
      containing the helper lipid dioleylphosphatidylethanolamine (DOPE) in their 
      membrane (216 +/- 42 pmol/well) were taken up to the most. Selected liposomes 
      were tested for their transcytotic transport across a MDCK monolayer. Liposomes 
      L4 containing equimolar DOPE and octadecyl-1,1-dimethylpiperidin-1-ium-4-yl 
      phosphate (OPP) were the most efficient vesicles for transcellular transport 
      resulting in 808 +/- 30 pmol calcein/cm(2) in the basal medium (28.1% of total 
      liposomal marker added). Transcytosis was positively correlated with membrane 
      fluidity in the outer part of the bilayer, as electron paramagnetic resonance 
      measurements revealed. We expect that an increase in membrane fluidity of 
      vesicles should also improve the restricted transport of hydrophilic drugs across 
      the blood-brain barrier.
FAU - Orthmann, Andrea
AU  - Orthmann A
AD  - Experimental Pharmacology, Max Delbruck Center for Molecular Medicine, 
      Robert-Rossle-Str. 10, 13125 Berlin-Buch, Germany.
FAU - Zeisig, Reiner
AU  - Zeisig R
FAU - Koklic, Tilen
AU  - Koklic T
FAU - Sentjurc, Marjeta
AU  - Sentjurc M
FAU - Wiesner, Burkhard
AU  - Wiesner B
FAU - Lemm, Margit
AU  - Lemm M
FAU - Fichtner, Iduna
AU  - Fichtner I
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - United States
TA  - J Pharm Sci
JT  - Journal of pharmaceutical sciences
JID - 2985195R
RN  - 0 (Drug Carriers)
RN  - 0 (Fluoresceins)
RN  - 0 (Fluorescent Dyes)
RN  - 0 (Unilamellar Liposomes)
RN  - V0YM2B16TS (fluorexon)
SB  - IM
MH  - Animals
MH  - Biological Transport
MH  - Cell Line
MH  - Cell Membrane/drug effects/metabolism
MH  - Dogs
MH  - Drug Carriers/*chemistry/pharmacokinetics
MH  - Drug Compounding
MH  - Electron Spin Resonance Spectroscopy
MH  - Epithelial Cells/drug effects/*metabolism
MH  - Fluoresceins/administration & dosage
MH  - Fluorescent Dyes/administration & dosage
MH  - *Membrane Fluidity
MH  - Microscopy, Confocal
MH  - Microscopy, Fluorescence
MH  - Nanoparticles/*chemistry
MH  - Unilamellar Liposomes/*chemistry/pharmacokinetics
EDAT- 2009/12/17 06:00
MHDA- 2010/06/26 06:00
CRDT- 2009/12/17 06:00
PHST- 2009/12/17 06:00 [entrez]
PHST- 2009/12/17 06:00 [pubmed]
PHST- 2010/06/26 06:00 [medline]
AID - S0022-3549(15)32646-0 [pii]
AID - 10.1002/jps.22001 [doi]
PST - ppublish
SO  - J Pharm Sci. 2010 May;99(5):2423-33. doi: 10.1002/jps.22001.