Effect of 1-hydroxyethylidene-1,1-bisphosphonate on membrane-mediated calcium phosphate formation in model liposomal suspensions. 1994

D Skrtic, and E D Eanes
National Institute of Dental Research's Research Associate Program, National Institute of Standards and Technology, Gaithersburg, MD 20899.

The bisphosphonate, 1-hydroxyethylidene-1,1-bisphosphonate (HEBP), was examined for its effect on calcium phosphate precipitation in pH 7.4, 22 degrees C suspensions of 7:2:1 PC:phosphatidylcholine (PC):dicetylphosphate (DCP):cholesterol (Chol) and 7:1:1 PC:phosphatidylserine (PS):Chol liposomes. HEBP (0.5-50 mumol/l) in the suspending medium had little, if any, effect on precipitation that formed inside phosphate-rich (50 mmol/l) aqueous interiors of liposomes as a result of ionophore (X-537A) driven 2.25 mmol/l Ca2+ influxes from the medium. On the other hand, HEBP had a significant negative impact on the subsequent spread of the precipitate into the surrounding medium when the latter was made metastable with 1.5 mmol/l total inorganic phosphate (PO4). The inhibitory effect of HEBP was more strongly felt in the 7PC:1PS:1Chol liposomal suspensions, with only 1 mumol/l HEBP needed to effectively block extraliposomal precipitation compared to 7.5 mumol/l for 7PC:2DCP:1Chol suspensions. Direct encapsulation of HEBP (1-1000 mumol/l) together with PO4 in the aqueous cores of 7PC:2DCP:1Chol liposomes reduced somewhat (approximately 30%) intraliposomal yields and delayed but did not block extraliposomal precipitate development. These results provide a possible physicochemical explanation for the suppression of matrix vesicle initiated mineralization in ectopically-induced osteoid tissue of HEBP treated mice [1]. In particular, the liposome results suggest that membrane phosphatidylserine interactions with mineral may enhance HEBP's effectiveness in vivo.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
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
D011232 Chemical Precipitation The formation of a solid in a solution as a result of a chemical reaction or the aggregation of soluble substances into complexes large enough to fall out of solution. Precipitation, Chemical
D002130 Calcium Phosphates Calcium salts of phosphoric acid. These compounds are frequently used as calcium supplements. Phosphates, Calcium
D006863 Hydrogen-Ion Concentration The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH pH,Concentration, Hydrogen-Ion,Concentrations, Hydrogen-Ion,Hydrogen Ion Concentration,Hydrogen-Ion Concentrations
D012968 Etidronic Acid A diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover. EHDP,Ethanehydroxydiphosphonate,Etidronate,Etidronate Disodium,Sodium Etidronate,(1-hydroxyethylene)diphosphonic acid,(1-hydroxyethylene)diphosphonic acid, Tetrapotassium Salt,1,1-hydroxyethylenediphosphonate,1-Hydroxyethane-1,1-Diphosphonate,1-Hydroxyethylidene-1,1-Bisphosphonate,Dicalcium EHDP,Dicalcium Etidronate,Didronel,Disodium 1-Hydroxyethylene Diphosphonate,Disodium Etidronate,Ethanehydroxyphosphate,Etidronate, Tetrapotassium Salt,HEDP,HEDSPA,Hydroxyethanediphosphonate,Hydroxyethylidene Diphosphonic Acid,Phosphonic acid, (1-hydroxyethylidene)bis-, disodium salt,Xidifon,Xidiphon,Xydiphone,1 Hydroxyethane 1,1 Diphosphonate,1 Hydroxyethylidene 1,1 Bisphosphonate,1,1 hydroxyethylenediphosphonate,1-Hydroxyethylene Diphosphonate, Disodium,Diphosphonate, Disodium 1-Hydroxyethylene,Diphosphonic Acid, Hydroxyethylidene,Disodium 1 Hydroxyethylene Diphosphonate,EHDP, Dicalcium,Etidronate, Dicalcium,Etidronate, Disodium,Etidronate, Sodium,Salt Etidronate, Tetrapotassium,Tetrapotassium Salt Etidronate

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