Association of liposomes containing a soybean-derived sterylglucoside mixture with rat primary cultured hepatocytes. 1998

K Shimizu, and Y Maitani, and N Takahashi, and K Takayama, and T Nagai
Department of Pharmaceutics, Hoshi University, Tokyo, Japan.

Dipalmitoylphosphatidylcholine (DPPC) and cholesterol (Ch) liposomes containing a soybean-derived sterylglucoside mixture (SG) (SG-liposomes) are effective for targeting hepatocytes in mice. We investigated uptake of SG-liposomes to hepatocytes compared with that via the galactose receptor. The association of SG-liposomes entrapping calcein was examined at 4 degrees C or 37 degrees C, changing incubation time and the SG concentration of the liposomes, and using the inhibitor on the galactose receptor in rat primary cultured hepatocytes. The amount of liposomes recovered with hepatocytes was determined by measuring the concentration of calcein and imaged with confocal laser scanning microscopy in the cultured cells. The association of SG-liposomes at 4 degrees C was significantly decreased compared with that at 37 degrees C as that of liposomes containing lactosylceramide (LC) (LC-liposomes) that were already known to be taken up by hepatocytes via the asialoglycoprotein receptor. While the association of SG-liposomes at both 4 degrees C and 37 degrees C increased with the increase of incubation time, the association of SG-liposomes at 37 degrees C was almost saturated after 1 h. The association of SG-liposomes pretreated with concanavalin A was significantly decreased (to about 40% of that without pretreatment at 37 degrees C) and was at the same level as the association of SG-liposomes and non-SG-liposomes at 4 degrees C. The association of the SG-liposomes by hepatocytes incubated for I h at 37 degrees C was almost saturated at about 2.0 nmol SG/mg protein. The association of the SG-liposomes with hepatocytes was not inhibited in the presence of LC-liposomes. The affinity of the galactose residue for hepatocytes appeared to be similar to that of the glucose residue in the liposomes, because the amount of sugar residue and the association of SG-liposomes and LC-liposomes were almost the same values. These results suggest that SG-liposomes may be associated with hepatocytes not by a galactose receptor-mediated endocytosis.

UI MeSH Term Description Entries
D008081 Liposomes Artificial, single or multilaminar vesicles (made from lecithins or other lipids) that are used for the delivery of a variety of biological molecules or molecular complexes to cells, for example, drug delivery and gene transfer. They are also used to study membranes and membrane proteins. Niosomes,Transferosomes,Ultradeformable Liposomes,Liposomes, Ultra-deformable,Liposome,Liposome, Ultra-deformable,Liposome, Ultradeformable,Liposomes, Ultra deformable,Liposomes, Ultradeformable,Niosome,Transferosome,Ultra-deformable Liposome,Ultra-deformable Liposomes,Ultradeformable Liposome
D008099 Liver A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances. Livers
D008297 Male Males
D010840 Phytosterols A class of organic compounds known as sterols or STEROIDS derived from plants. Plant Sterols,Phytosteroid,Phytosteroids,Phytosterol,Plant Steroid,Plant Steroids,Plant Sterol,Steroid, Plant,Steroids, Plant,Sterol, Plant,Sterols, Plant
D011956 Receptors, Cell Surface Cell surface proteins that bind signalling molecules external to the cell with high affinity and convert this extracellular event into one or more intracellular signals that alter the behavior of the target cell (From Alberts, Molecular Biology of the Cell, 2nd ed, pp693-5). Cell surface receptors, unlike enzymes, do not chemically alter their ligands. Cell Surface Receptor,Cell Surface Receptors,Hormone Receptors, Cell Surface,Receptors, Endogenous Substances,Cell Surface Hormone Receptors,Endogenous Substances Receptors,Receptor, Cell Surface,Surface Receptor, Cell
D002478 Cells, Cultured Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others. Cultured Cells,Cell, Cultured,Cultured Cell
D003208 Concanavalin A A MANNOSE/GLUCOSE binding lectin isolated from the jack bean (Canavalia ensiformis). It is a potent mitogen used to stimulate cell proliferation in lymphocytes, primarily T-lymphocyte, cultures.
D004337 Drug Carriers Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers. Drug Carrier
D005960 Glucosides A GLYCOSIDE that is derived from GLUCOSE. Glucoside
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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