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    • 8. 发明专利
    • Polylactide nanoparticles
    • IN8036DE2008A
    • 2009-03-20
    • IN8036DE2008
    • 2008-09-24
    • LOHMANN THERAPIE SYST LTS
    • GELPERINA SVETLANAMAKSIMENKO OLGAKREUTER JOERGKHALANSKIY ALEXANDER
    • Drug delivery system for the targeted supply of a pharmaceutical substance to the central nervous system of a mammal over the blood-brain barrier, comprises: nanoparticles of poly(DL-lactide) and/or poly(DL-lactide-co-glycolide)(PLGA); and at least a pharmaceutical substance, which is absorbed or incorporated in or adsorbed at the nanoparticles, where the drug deliver system contains d-alpha tocopheryl polyethylene glycol succinate (TPGS) or exhibits a coat on a surface-active material, which is deposited on the nanoparticles that are loaded with the active substance. Drug delivery system for the targeted supply of a pharmaceutical substance to the central nervous system of a mammal over the blood-brain barrier, comprises: nanoparticles of poly(DL-lactide) and/or poly(DL-lactide-co-glycolide) (PLGA); and at least a pharmaceutical substance, which is absorbed or incorporated in or adsorbed at the nanoparticles, where the drug deliver system contains d-alpha tocopheryl polyethylene glycol succinate (TPGS) or exhibits a coat on the surface-active material Pluronic 188 (RTM: Non-ionic block copolymers based on ethylene oxide and propylene oxide) or Poloxamer 188 (RTM: Non-ionic block copolymers based on ethylene oxide and propylene oxide) (A), which is deposited on the nanoparticles that are loaded with the active substance. Independent claims are included for: (1) a procedure for the production of drug delivery system for the targeted supply of a pharmaceutical substance to the central nervous system of a mammal over the blood-brain barrier, comprising dissolving poly(DL-lactide) and/or poly(DL-lactide-co-glycolide) as well as at least a pharmaceutical substance and alternatively a lipid compound in an organic solvent, in order to obtain an organic phase; pouring the organic phase into an aqueous solution containing TPGS; emulsifying the mixture, in order to receive a primary emulsion; homogenizing the primary emulsion; removing the organic solvent from the primary emulsion; and filtering the resulting nano-suspension, which contains nanoparticles loaded with the active substance; and (2) a procedure for the treatment of an disease or a disorder of the central nervous system of a mammal, comprising preparing nanoparticles loaded with the active substance made of poly(DL-lactide) and/or poly(DL-lactide-co-glycolide); covering of the PLGA nano particle loaded with the active substance with (A); administrating the nanoparticles, which are loaded with the active substance and covered with (A), to the blood circulatory system of a mammal; and releasing the active substance, so that it can unfold its pharmacological effect. ACTIVITY : CNS-Gen; Cytostatic. MECHANISM OF ACTION : None given.