Publications by Type: Patents

1999
Desai NP, Tao C, Yang A, Louie L, Zheng T, Yao Z, Soon-Shiong P, Magdassi S.; 1999. Protein stabilized pharmacologically active agents, methods for the preparation thereof and methods for the use thereof.Abstract
In accordance with the present invention, there are provided compns. and methods useful for the in vivo delivery of substantially water-insol. pharmacol. active agents (such as the anticancer drug paclitaxel) in which the pharmacol. active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacol. active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diam. of less than about 1 μm. The use of specific compn. and prepn. conditions (e.g., addn. of a polar solvent to the org. phase), and careful selection of the proper org. phase and phase fraction, enables the reproducible prodn. of unusually small nanoparticles of less than 200 nm diam., which can be sterile-filtered. The particulate system produced according to the invention can be converted into a redispersible dry powder comprising nanoparticles of water-insol. drug coated with a protein, and free protein to which mols. of the pharmacol. agent are bound. This results in a unique delivery system, in which part of the pharmacol. active agent is readily bioavailable (in the form of mols. bound to the protein), and part of the agent is present within particles without any polymeric matrix therein. [on SciFinder(R)]
Magdassi S, Yang A, Tao C, Desai NP, Yao Z, Soon-Shiong P.; 1999. Total nutrient admixtures as stable multicomponent liquids or dry powders and methods for preparation.Abstract
Stabilized total nutrient admixt. (TNA) compns. are useful for the in vivo parenteral delivery of pharmacol. acceptable lipids or fats. The lipid or fat is contained within a protein walled shell. Thus, a TNA compn. using human serum albumin (HSA) as a stabilizer is prepd. as a convenient three-in-one formulation (i.e., contg. a fat emulsion, dextrose, and amino acids plus electrolytes). This "three-in-one" formulation can be prepd. in liq. form or in dry form (comprising submicron-sized nanoparticles). The dried material is stable, even under long term storage, and is easily reconstituted immediately before use by simply adding sterile water (with or without vitamin supplementation). This serves to rehydrate the powder into a TNA suitable for injection. The long shelf life, ease of reconstitution, and single-component injectability provide significant cost savings, as such compns. can be reconstituted and administered safely, even in the home. In addn., HSA, the stabilizing agent of choice, is known to improve survival and wellness when given as a supplement to patients receiving conventional forms of total nutrient admixts. [on SciFinder(R)]
Maor Z, Yehuda S, Magdassi S, Kogan A.; 1999. A gel composition for skin care and protection and a method for preparation thereof.Abstract
The present invention relates to a gel compn. useful for skin care and protection comprising up to 80 % wt./wt. Dead Sea water, hydrophobic and/or hydrophilic active agents, solubilizers, gelling agents or viscosity modifiers and water to complete up to 100 %. Preferably, the compn. is a clear liq. gel. In the compn. of the present invention the hydrophobic active agents may be vegetable oils, free fatty acids or vitamins, or any combination thereof and the hydrophilic active agent may be humectants, α-hydroxy acids, anti irritant agents, plant exts., moisturizing agents or hydrolyzed plant proteins or any combination thereof. The gel may further comprise antioxidants and fragrances. A compn. contained Dead Sea water 75.0, oleth 20 3.0, glycereth 26 2.0, hydroxyethyl cellulose 0.8, tocopheryl acetate 0.3, lavender oil 0.3, BHA 0.1 and deionized water to 100%. [on SciFinder(R)]
Desai NP, Soon-Shiong P, Magdassi S, Sahadevan DC.; 1999. Novel formulations of pharmacological agents, methods for the preparation thereof and methods for the use thereof.Abstract
In accordance with the present invention, there are provided compns. and methods useful for the in vivo delivery of substantially water-insol. pharmacol. active agents (such as the anticancer drug paclitaxel) in which the pharmacol. active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacol. active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diam. of <1 μm. The use of specific compn. and prepn. conditions (e.g., addn. of a polar solvent to the org. phase), and careful selection of the proper org. phase and phase fraction, enables the reproducible prodn. of unusually small nanoparticles of <200 nm diam., which can be sterile-filtered. The particulate system produced can be converted into a redispersible dry powder comprising nanoparticles of water-insol. drug coated with a protein, and free protein to which mols. of the pharmacol. agent are bound. This results in a unique delivery system, in which part of the pharmacol. active agent is readily bioavailable (in the form of mols. bound to the protein), and part of the agent is present within particles without any polymeric matrix therein. [on SciFinder(R)]
1998
Magdassi S, Yang A, Tao C, Desai NP, Yao Z, Soon-Shiong P.; 1998. Total nutrient admixtures as stable multicomponent liquids or dry powders and methods for the preparation thereof.Abstract
Disclosed are stabilized total nutrient admixt. (TNA) compns. useful for parenteral delivery of pharmacol. acceptable lipids or fats as well as methods for the prepn. thereof. In particular, the pharmacol. acceptable lipid or fat is contained within a protein-walled shell. In a particular embodiment of the invention, a TNA compn. using human serum albumin (HSA) as a stabilizer has been prepd. as a convenient three-in-one formulation (i.e., contg. a fat emulsion, dextrose, and amino acids plus electrolytes). This "three-in-one" formulation can be prepd. in liq. form or in dry form (comprising submicron-sized nanoparticles). The dried material is stable, even under long-term storage, and is easily reconstituted immediately before use by simply adding sterile water (with or without vitamin supplementation). This serves to rehydrate the powder into a TNA suitable for injection. The long-shelf life, ease of reconstitution, and single-component injectability of invention compns. provide significant cost savings, as such compns. can be reconstituted and administered safely, even in the home. In addn., HSA, the stabilizing agent of choice for use in the practice of the present invention, has been shown to improve survival and wellness when given as a supplement to patients receiving conventional forms of total nutrient admixts. Thus, 15 mL of 10 % amino acid soln. (FreAmine III), 4.3 mL of 70 % dextrose soln., 0.5 mL phosphate buffer, 0.4 mL KCl (2 M), NaCl (4 M), 0.5 mL MgSO4 (0.406 M), 0.5 mL Na citrate (10 %), 0.5 mL Ca gluconate (0.46 M) were mixed with 0.25 g of HSA until a clear soln. was obtained. The soln. was filtered and 2.5 mL soybean oil was added to the aq. soln. and the mixt. was homogenized (condition was detailed). The emulsion was stored under N in a polypropylene test tube for 1 wk at 4°, followed by one day at room temp.; the droplet size was not changed and there were no signs of oil sepn. or creaming. [on SciFinder(R)]
Magdassi S, Mumcuoglu K, Bach U, Rosen Y.; 1998. Method of making positively charged microcapsules of emulsions of oils and its uses.Abstract
The invention relates to a process for prepg. a chitosan-contg. microcapsules and emulsions of an oil including the steps of (a) forming an oil-in-water emulsion by homogenizing the oil into an aq. soln. contg. an anionic emulsifier; and (b) adding to the emulsion obtained in (a) an aq. chitosan soln. while continuously homogenizing the mixt. to give a stable emulsion, which is converted into microcapsules by using the proper electrolyte and pH changes. Also encompassed are prepns. including as active ingredient a lice repelling agent, vitamin E or a UV radiation photoprotectant. The prepns. may be sustained-release or long-acting prepns. Rosemary oils were dropwise added into a lecithin soln. in water in a homogenizer to obtain a white emulsion, to which a chitosan soln. (prepd. by dissolving chitosan into a citric acid soln.) was added. The final compn. (pH 3.5) contained rosemary oil 15, chitosan 0.5, citric acid 5, lecithin 0.35, and water 79.15 %. An excellent lice repellency of the emulsion was demonstrated. [on SciFinder(R)]
Magdassi S, Desai N, Ferreri K, Soon-Shiong P.; 1998. Methods for the production of protein particles useful for delivery of pharmacological agents.Abstract
A method has been developed for the formation of submicron particles (nanoparticles) by heat-denaturation of proteins (such as human serum albumin) in the presence of multivalent ions (such as calcium). Also provided are novel products produced by the invention method. An appropriate concn. of multivalent ions, within a relatively narrow range of concns., induces the pptn. of protein in the form of colloidal particles, at a temp. which is well below the heat denaturation temp. of the protein (as low as 60 °C for serum albumin). Temps. at which invention method operates are sufficiently low to permit incorporation of other mols. (e.g., by co-pptn.), into submicron particles according to the invention, including compds. which cannot withstand high temps. Invention methods facilitate the prodn. of protein nanoparticles and microparticles contg. various mols. (such as nucleic acids, oligonucleotides, polynucleotides, DNA, RNA, polysaccharides, ribozymes, pharmacol. active compds., and the like) useful for therapeutic, diagnostic and other purposes. The addn. of multivalent cations serves both to induce pptn., and to allow linking of neg. charged mols., such as DNA, to the neg. charged protein. Microparticles and nanoparticles were formed from albumin in the presence of CaCL2. [on SciFinder(R)]
Desai NP, Tao C, Yang A, Louie L, Zheng T, Yao Z, Soon-Shiong P, Magdassi S.; 1998. Protein stabilized pharmacologically active agents, methods for the preparation thereof and methods for the use thereof.Abstract
Compns. are provided for the in vivo delivery of substantially water-insol. pharmacol. active agents (such as the anticancer drug paclitaxel) in which the pharmacol. active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacol. active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diam. of less than about 1 μ. The use of specific compn. and prepn. conditions (e.g., addn. of a polar solvent to the org. phase), and careful selection of the proper org. phase and phase fraction, enables the reproducible prodn. of unusually small nanoparticles of less than 200 nm diam., which can be sterile-filtered. The particulate system produced according to the invention can be converted into a redispersible dry power comprising nanoparticles of water-insol. drug coated with a protein, and free protein to which mols. of the pharmacol. agent are bound. This results in a unique delivery system, in which part of the pharmacol. active agent is readily bioavailable (in the form of mols. bound to the protein), and part of the agent is present within particles without any polymeric matrix therein. Albumin nanoparticles contg. paclitaxel were prepd. by high pressure homogenization. [on SciFinder(R)]
1996
Magdassi S, Mumcuoglu K, Bach U.; 1996. Method of preparing natural oil-containing emulsions and microcapsules and its uses.Abstract
The invention relates to a process for prepg. a chitosan-contg. aq. emulsion of an oil comprising the steps of (a) forming an oil-in-water emulsion by homogenizing the oil into an aq. soln. contg. an anionic emulsifier; and (b) adding to the emulsion obtained in (a) an aq. chitosan soln. while continuously homogenizing the mixt. to give a stable emulsion. In further aspect the invention relates to a process for the microcapsulation of fine oil droplets. The invention also relates to sustained-release biodegradable prepns. comprising as active ingredient vitamin E or a UV radiation photoprotectant or a lice repelling agent comprising at least one natural oil or natural oil component thereof and further comprising an anionic emulsifier and chitosan. A lice-repelling emulsion contained rosemary oil 15, chitosan 0.5, citric acid 5, lecithin 0.35, and water 79.15%. The final pH of the emulsion was 3.5 and the emulsion was stable for ≥8 mo at room temp. When the emulsion was applied to human hair fibers, the chitosan microcapsules contg. rosemary oil adhered well to the fiber. [on SciFinder(R)]
Eyal AM, Kotlyar S, Apfelbaum F, Magdassi S, Braun S.; 1996. Process for the preparation of long-chain alkyl glycosides.Abstract
The invention provides a process for the prepn. of long-chain alkyl glycosides, comprising reacting a glucose-contg. reactant and a C8-C18 fatty alc. in the presence of a glucosidase and a reaction promoter effective to promote the formation of the alkyl glycoside when the promoter is present in an amt. of <∼50% of the total reaction mixt. [on SciFinder(R)]
1995
Magdassi S, Rones ZZ, Linevitz M, Shanberg O.; 1995. Method and pharmaceutical compositions for drug targeting.Abstract
A pharmaceutical compn. comprising an oil/water emulsion wherein the oil droplets contain a drug in dissolved or dispersed or solubilized form. The droplets are further coated with adsorbed native or modified antibodies which provide targeting of the droplets and the drug. The process for prepg. this compn. comprises the steps of dissolving or dispersing a drug in an oil phase, prepg. an oil/water emulsion, obtaining surface-active antibodies by chem. or phys. attachment of hydrophobic groups to the antibodies, and mixing the surface-active antibody with the emulsion. The targeting of emulsion droplets to specific cells was demonstrated by using herpes virus (HSV-1) cells. [on SciFinder(R)]
Magdassi S, Rones ZZ, Toledano O.; 1995. Antibody aggregates and hydrophobic drug or marker molecule pharmaceutical and diagnosis compositions for drug targeting.Abstract
The new pharmaceutical and diagnostic compns. comprise antibody-aggregates and hydrophobic drug or marker mols. The drug or marker mols. are solubilized inside micelle-like antibody-aggregates. In a process for prepg. such types of compns., hydrophobic residues are attached to the antibodies in the presence of a surface active agent. After removal of this agent the hydrophobic drug or marker mols. are solubilized inside the resulting antibody aggregates. A method for targeting mols. towards specific cells and sites within a living body is also disclosed. [on SciFinder(R)]
1990
Magdassi S.; 1990. Manufacture of colored contact lens.Abstract
Opaque contact lenses capable of imparting an apparent color modification to the wearer's iris comprises a polymer lens body and solid latex polymer particles directly bound to at least a portion of a surface of the lens. The invention method does not need for turbidity agent and binding polymer. A fully soaked lens was mounted on the index table of a transfer-pad printer and left to allow a portion of the water to evap. from the lens; an ink block contg. 40% ink and 60% HA-24 (latex from Rohm and Hass) was used for tinting the contact lens; after imprinting, the lenses are placed in an oven for 30-45 min at 80-95°. A schematic illustration of the tinting setup is given. [on SciFinder(R)]
1989
Shoshan S, Magdassi S, Michaeli D.; 1989. Collagen products, processes for the preparation thereof and pharmaceutical compositions containing the same.Abstract
A storage-stable lyophilized collagen product comprises acid-sol. purified native collagen in combination with platelet growth factors. A pharmaceutical compn. for enhancing wound healing comprises an aq. soln. of water sol. acid-sol. purified native collagen and platelet derived growth factors. [on SciFinder(R)]

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