Online citations, reference lists, and bibliographies.
← Back to Search

Lactose-carrying Polystyrene As A Drug Carrier : Investigation Of Body Distributions To Parenchymal Liver Cells Using 125I-labelled Lactose-carrying Polystyrene

Goto Mitsuaki, Yura Hirohumi, Chang Chia-Wun, K. Akira, Shinoda Tatsuki, Maeda Atsushi, Kojima Seiki, Kobayashi Kazukiyo, Akaike Toshihiro
Published 1994 · Chemistry

Cite This
Download PDF
Analyze on Scholarcy
Share
Directed toward pharmacological applications of lactose-carrying polystyrene, (poly (N-p-vinylbenzyl-O-β-D-galactopyranosyl-(l→4)-D-gluconamide), PVLA), its body distribution, clearance from blood and specific binding to receptors have been investigated using radiolabelled PVLA. 125I-Labelled PVLA was prepared via copolymerization of N-p-vinylbenzyl-O-β-D-galactopyranosyl-(l→4)-D-gluconamide (VLA) with 10 mol% of 4-(2-propenyl)phenyl acetate followed by radiolabelling of the latter component. When 125I-labelled PVLA was injected into rats through their tail veins, the radioactivity was distributed highly to liver, less to thyroid gland, cecum-large intestine, urine, feces and blood, and much less to lung, heart, kidney, spleen, pancreas, small intestine and urinary bladder. Its concentration to liver was visible by whole-body autoradiography. It was clarified that about 97% of PVLA was distributed to parenchymal liver cells and only 3% to nonparenchymal liver cells. The radioactivity in blood was decreased with time according to a biexponential curve. A two open compartment model is proposed on the basis of the pharmacokinetic analysis of the equation, which elucidated that PVLA migrated rapidly from blood to parenchymal liver cells. Specific binding between 125I-labelled PVLA and asialoglycoprotein receptors on parenchymal liver cells was demonstrated by its inhibition with asialofetuin. The bond dissociation constant estimated by Scatchard analysis was Kd=1.4x10-9 M. The binding was as strong as those of several naturally occurring asialoglycoproteins. These properties of PVLA, as liver-specific targeting materials using galactose ligands as recognition signals to asialoglycoprotein receptors, are discussed with the conformational structures of PVLA which can carry drugs in their hydrophobic regions.
This paper references
10.1111/j.1749-6632.1949.tb27297.x
THE ATTRACTIONS OF PROTEINS FOR SMALL MOLECULES AND IONS
G. Scatchard (1949)
Receptor-mediated gene delivery in vivo. Partial correction of genetic analbuminemia in Nagase rats.
G. Wu (1991)
A new concept for macromolecular therapeutics in cancer chemotherapy: mechanism of tumoritropic accumulation of proteins and the antitumor agent smancs.
Y. Matsumura (1986)
10.1016/0005-2736(87)90073-3
A newly developed immunoliposome--an egg phosphatidylcholine liposome coated with pullulan bearing both a cholesterol moiety and an IgMs fragment.
J. Sunamoto (1987)
Characterization and anticancer activity of the micelle-forming polymeric anticancer drug adriamycin-conjugated poly(ethylene glycol)-poly(aspartic acid) block copolymer.
M. Yokoyama (1990)
10.1002/MARC.1986.030071005
Enhanced adhesion and survival efficiency of liver cells in culture dishes coated with a lactose‐carrying styrene homopolymer
A. Kobayashi (1986)
10.1177/088391159200700201
In vivo Fate of Repeat-Unit-Radiolabelled Poly(β-malic acid), a Potential Drug Carrier
P. Fournie (1992)
10.1126/SCIENCE.2218494
New methods of drug delivery.
R. Langer (1990)
10.4052/TIGG.4.251
Perspective of Glycotechnology
Y. Lee (1992)
10.1246/CL.1992.123
Model study of hepatocyte targeting polymeric super molecular assembly as drug carrier
M. Goto (1992)
10.1042/BJ0890114
THE PREPARATION OF I-131-LABELLED HUMAN GROWTH HORMONE OF HIGH SPECIFIC RADIOACTIVITY.
F. Greenwood (1963)
10.1073/PNAS.88.13.5572
Delivery of macromolecules into living cells: a method that exploits folate receptor endocytosis.
C. P. Leamon (1991)
10.1021/BI00403A008
Evidence for targeted gene delivery to Hep G2 hepatoma cells in vitro.
G. Wu (1988)
10.1007/978-1-4612-5186-6_11
Macromolecules as Drug Delivery Systems
H. Sezaki (1985)
Human hepatic lectin. Physiochemical properties and specificity.
J. Baenziger (1980)
10.1295/POLYMJ.17.567
Synthesis and Functions of Polystyrene Derivatives Having Pendant Oligosaccharides
K. Kobayashi (1985)
10.1096/fasebj.6.13.1397841
Biochemistry of carbohydrate‐protein interaction 1
Y. Lee (1992)
10.1016/0092-8674(80)90371-2
Galactose and N-acetylgalactosamine-specific endocytosis of glycopeptides by isolated rat hepatocytes
J. Baenziger (1980)
10.1016/0006-2952(90)90293-T
The pharmacokinetics of polymer-bound adriamycin.
L. Seymour (1990)
10.1021/BC00013A008
Synthesis, conformation, biodistribution, and in vitro cytotoxicity of daunomycin-branched polypeptide conjugates.
F. Hudecz (1992)
10.1016/0006-291X(92)91182-P
Receptor-mediated formation of multilayer aggregates of primary cultured adult rat hepatocytes on lactose-substituted polystyrene.
S. Tobe (1992)
10.1111/j.2042-7158.1992.tb14354.x
Accumulation of Polyvinylpyrrolidone within the Inflamed Paws of Adjuvant‐induced Arthritic Rats
L. Seale (1992)



This paper is referenced by
10.1016/S0378-5173(02)00336-8
Development of a polymeric nanoparticulate drug delivery system. In vitro characterization of nanoparticles based on sugar-containing conjugates.
I. Kim (2002)
10.1016/J.REACTFUNCTPOLYM.2012.06.019
Preparation and characterization of polymeric nanoparticles composed of poly(dl-lactide-co-glycolide) and poly(dl-lactide-co-glycolide)-co-poly(ethylene glycol)-10%-Triblock end-capped with a galactose moiety
I. N. Peça (2012)
10.1093/JB/MVJ077
Interaction study between synthetic glycoconjugate ligands and endocytic receptors using flow cytometry.
H. Yura (2006)
10.1016/j.msec.2017.08.004
Albumin based versatile multifunctional nanocarriers for cancer therapy: Fabrication, surface modification, multimodal therapeutics and imaging approaches.
Ritu R. Kudarha (2017)
10.1021/la400144t
Synthesis and self-assembly of amphiphilic homoglycopolypeptide.
Vinita Dhaware (2013)
10.1016/0378-5173(95)00068-T
Effects of soybean-derived sterol and its glucoside mixtures added in dipalmitoylphosphatidylcholine liposomes on the blood circulation and hepatic cellular distribution in mice
K. Muramatsu (1995)
10.1111/j.1525-1594.2009.00746.x
Coatings of low-density lipoprotein and synthetic glycoconjugates as substrata for hepatocytes.
H. Yura (2009)
10.1002/adhm.201700306
Synthesis, Functionalization, and Design of Magnetic Nanoparticles for Theranostic Applications
Jalal Mosayebi (2017)
10.2967/jnumed.110.085167
Copolymer-Based Hepatocyte Asialoglycoprotein Receptor Targeting Agent for SPECT
W. Yang (2011)
10.1016/J.CARBPOL.2007.09.004
Preparation and characterization of galactosylated chitosan coated BSA microspheres containing 5-fluorouracil
C. Zhang (2008)
10.1002/APP.21975
Synthesis and characterization of chitosan derivatives carrying galactose residues
Can Zhang (2005)
10.5772/23372
Negative Impact of Paclitaxel Crystallization on Hydrogels and Novel Approaches for Anticancer Drug Delivery Systems
J. S. Castro (2011)
10.1016/J.IJPHARM.2005.02.027
Cellular recognition of paclitaxel-loaded polymeric nanoparticles composed of poly(gamma-benzyl L-glutamate) and poly(ethylene glycol) diblock copolymer endcapped with galactose moiety.
Y. Jeong (2005)
10.1007/s11095-006-9223-y
Functionalized Micellar Systems for Cancer Targeted Drug Delivery
Damon M Sutton (2006)
10.1016/S0142-9612(96)00138-X
Simple preparation of nanoparticles coated with carbohydrate-carrying polymers.
C. S. Cho (1997)
10.3109/10611869808997897
Disposition characteristics of glycosylated poly(amino acids) as liver cell-specific drug carrier.
K. Akamatsu (1998)
10.1016/S0142-9612(01)00129-6
Galactosylated alginate as a scaffold for hepatocytes entrapment.
Jun Yang (2002)
10.1002/MACP.201000007
Glycopolymers of Various Architectures—More than Mimicking Nature
B. Voit (2010)
10.1002/PI.1050
Regioselective end‐functionalization of polylactide oligomers with D‐glucose and D‐galactose
K. Bernard (2003)
Glycopolymer Polyelectrolyte Multilayers Based on Maltose-Modified Hyperbranched Poly(ethyleneimine) For Future Drug Delivery Coatings and Biomedical Applications
Samaa R. Salem (2015)
10.1080/107175499266896
Nanosphere Coated with Lactosyl-Polystyrene Polymer as a Targeting Carrier to Hepatocytes
Tatsuki Shinoda (1999)
10.1295/POLYMJ.31.970
Graft Copolymers Having Hydrophobic Backbone and Hydrophilic Branches XXI. Preparation of Galactose Surface-Accumulated Polystyrene Nanospheres and Their Interaction with Lectin
Toshiro Uchida (1999)
10.1002/CHIN.199901326
Progress in Structural Characterization of Functional Polysaccharides
K. Kajiwara (1999)
10.1002/JBM.A.10421
Visualization of specific interaction between biomimetic glycopolymer containing reducing glucose moiety and HepG2 cell mediated by GLUT-1.
Keun-Hong Park (2003)
10.1016/J.EJPB.2004.03.025
Delivery of all trans-retinoic acid (RA) to hepatocyte cell line from RA/galactosyl alpha-cyclodextrin inclusion complex.
S. Seo (2004)
10.1088/0957-4484/24/47/475103
Galactosylated manganese ferrite nanoparticles for targeted MR imaging of asialoglycoprotein receptor.
Seung-hyun Yang (2013)
10.1016/S0378-5173(03)00128-5
Development of polymeric nanoparticulate drug delivery systems: evaluation of nanoparticles based on biotinylated poly(ethylene glycol) with sugar moiety.
I. Kim (2003)
10.1002/MABI.200700157
Copolymers for hepatocyte-specific targeting carrying galactose and hydrophobic alkyl groups.
T. Hiratsuka (2008)
10.1016/j.jconrel.2018.06.026
Saccharides, oligosaccharides, and polysaccharides nanoparticles for biomedical applications
Farzad Seidi (2018)
10.1263/JBB.99.285
Specific interaction of mannosylated glycopolymers with macrophage cells mediated by mannose receptor.
Keun-Hong Park (2005)
10.1016/J.MSEC.2005.09.052
Receptor-mediated delivery of all-trans-retinoic acid (ATRA) to hepatocytes from ATRA-loaded poly(N-p-vinylbenzyl-4-o-β-d-galactopyranosyl-d-gluconamide) nanoparticles
Seog Jin Seo (2006)
REVIEW Polymeric micelles: authoritative aspects for drug delivery
Sushant S. Kulthe (2012)
See more
Semantic Scholar Logo Some data provided by SemanticScholar