Liposomes used for delivery of medications

IPC classes for russian patent Liposomes used for delivery of medications (RU 2424792):

A61K9/50 - Microcapsules (A61K0009520000 takes precedence);;

A61K9/127 -

A61K9 - Medicinal preparations characterised by special physical form

A61K47/44 - Oils, fats or waxes according to more than one of groups ; A61K0047020000-A61K0047420000

A61K47/36 - Polysaccharides; Derivatives thereof

A61K47/30 - Macromolecular compounds

A61K47/10 - Alcohols; Phenols; Salts thereof

A61K45/08 - Mixtures of an active ingredient and an auxiliary substance neither being chemically characterised, e.g. antihistaminicum and surface active substance

A61K36/24 - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J0003000000; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L)

A61K31/4375 -

A61K31/337 -

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FIELD: medicine, pharmaceutics.

SUBSTANCE: in claimed invention it suggested are liposome compositions, which contain substituted ammonia and/or polyanion and, optionally, desirable therapeutic agent or expressing contrast substance.

EFFECT: invention provides efficient method of obtaining liposome compositions.

141 cl, 40 tbl, 74 ex, 47 dwg

The text descriptions are given in facsimile form.

1. The composition for drug delivery or diagnostic compounds representing the liposome in an environment that has an internal space that is separated from the environment by a membrane comprising one or more lipids, and the inner space of the liposome contains a substituted ammonium having the formula
R₁-(R_2-)N⁺(R₃)-R₄
where N represents an ammonium nitrogen atom, each of R₁, R₂, R₃, R₄represents independently a hydrogen atom or an organic group having each independently not more than 8 carbon atoms and in General (in the aggregate) not more than 18 carbon atoms, inclusive, and at least one of R₁, R₂, R₃, R₄is an organic group, the organic group independently represents an alkyl, alkylidene, heterocyclic alkyl, cycloalkyl, aryl, alkenyl, cycloalkenyl or replacement derivative, optionally containing atoms S, O or N, form an ether, ester, thioester, amino or amide bond, and where at least three of R₁, R₂, R₃, R₄are organic groups, or at least one of the organic groups is a secondary or tertiary carbon atom directly linked to the ammonium nitrogen atom, and where the specified internal space is nstwo also includes anion.

2. The composition according to claim 1, characterized in that among the organic groups each independently contain not more than 6 carbon atoms.

3. The composition according to claim,1, wherein the organic groups together contain no more than 16 carbon atoms.

4. The composition according to claim 1, characterized in that the organic groups together contain no more than 12 carbon atoms.

5. The composition according to claim 1, characterized in that the substituted ammonium forms a true solution in water.

6. The composition according to claim,1, wherein virtually all of substituted ammonium contained in the inner space of the liposome.

7. The composition according to claim 1, characterized in that the substituted ammonium ion is pharmaceutically inert.

8. The composition according to claim 1, characterized in that the substituted ammonia selected from the group consisting of isopropylacrylamide, isopropylethylene, Diisopropylamine, tributylamine, dicyclohexylamine, morpholine, pyridinium, piperidine, pyrrolidine, piperazine, tributylamine, 2-ammonium-2-methylpropanol-1,2-ammonium-2-methylpropanol-1,3-Tris-(hydroxyethyl)-ammonium methane, N,N'-diethyl-ethanolamine, N,N',N"-Tris-(2-hydroxyethyl)ammonium, N,N'-bis-(2-hydroxyethyl)ethylamine, trimethylammonium, triethylamine, Diethylenetriamine, diisopropylethylamine, triisopropanolamine, N-methylmorpholine, 1-(2-hydroxyethyl)piperidine, 1-IU is iparralde, 1,4-dimethylpiperazine, Tetramethylammonium, tetraethylammonium and tetrabutylammonium.

9. The composition according to claim 1, characterized in that the concentration of the substituted ammonium in the inner space of the liposomes is higher than the concentration of the substituted ammonium in the medium containing liposomes.

10. The composition according to claim 1, characterized in that the concentration of the substituted ammonium in the inner space is at least about 0.05 M, 0.1 M, 0.2 M, 0.5 M, 0.6 M or 0.7 M

11. The composition according to claim 10, characterized in that the concentration of the substituted ammonium in the inner space of approximately 0,65 M

12. The composition according to claim 1, characterized in that the anion is polyaniondivalent a monosaccharide or polyaniondivalent a disaccharide.

13. The composition for drug delivery or diagnostic compounds representing the liposome in an environment that has an internal space that is separated from the environment by a membrane comprising one or more lipids, and an internal space includes an anion selected from polianilinovykh of monosaccharide or polianilinovykh disaccharide, and the liposome comprises a transmembrane gradient, effective for holding the substance inside the liposomes.

14. The composition according to item 13, wherein the transmembrane ion gradient is a gradient, the gradient of ammonium ion, the pH of radiant, the gradient of the electrochemical potential gradient of solubility or the gradient of the substituted ammonium ion containing at least one C-N bond.

15. Composition according to any one of claims 1 to 11, 13, 14, characterized in that prinivilbuy monosaccharide or prinivilbuy disaccharide is associated with at least two selenoenzyme functional groups.

16. The composition according to item 15, wherein at least one strong base functional group is an ester of sulfuric acid, ether phosphoric acid ester of boric acid, sulfonic group, phosphonic acid group, a group thiocarbonic acid or group dithiocarbonic acid.

17. The composition according to item 15, characterized in that the said monosaccharide is selected from the group consisting of arabinose, ribose, xylose, glucose, galactose, sorbose and fructose; and the specified disaccharide selected from the group consisting of maltose, sucrose, lactose and trehalose.

18. The composition according to item 15, wherein prinivilbuy disaccharide is polysulfonamide sucrose having from 3 to 8 of sulfate groups in the molecule.

19. The composition according to p, characterized in that poliuretonovaya sucrose is sharepointserver.

20. The composition according to item 15, wherein the concentration of polianilinovykh monosaccharide is or polianilinovykh disaccharide inside liposomes is, at least about 0,05, 0,1, 0,2, 0,5, 0,6 0,7 or 1.0 gram equivalent/L.

21. The composition according to claim 20, characterized in that the concentration polianilinovykh of monosaccharide or polianilinovykh disaccharide inside the liposomes is about 0.65 gram equivalent/l, or about 1.0 gram equivalent/L.

22. The composition according to claim 1, characterized in that it further contains a fully cationic substance, therapeutic agent or the detected token.

23. The composition according to item 22, wherein the specified fully cationic substance, therapeutic agent or the detected marker is contained in the inner space in a concentration that exceeds the concentration of these substances in the environment.

24. The composition according to item 22, wherein the environment is almost free from these substances.

25. The composition according to item 22, wherein the molar ratio of these substances to the total number of lipids is about 0.05, about 0.1, about 0.2, about 0.3, about 0.5, about 0.7, or about 1.0.

26. The composition according to item 22, wherein therapeutic agent is an antimicrobial therapeutic agent, an antiviral therapeutic agent or antineoplastics therapeutic agent.

27. The composition according to item 22, wherein therapeutic agent is an aminoglycoside antibiotic or derivative f is originalone.

28. The composition according to p, wherein therapeutic agent is selected from the group comprising: a topoisomerase inhibitor, an inhibitor farnesyltransferase, a tyrosine kinase inhibitor, an inhibitor of cyclin-dependent kinase, a phosphatase inhibitor, inhibitor euroracing, microcalorimetry agent, microtubuleassociated agent, an alkylating agent, an enzyme, an enzyme inhibitor, an inhibitor of histone-deacetylase, an antimetabolite, a receptor-binding agent, a hormone antagonist, a hormone, a nucleotide or polynucleotide.

29. The composition according to p, characterized in that antineoplastics therapeutic agent selected from the group including derivative anthracycline, derived camptothecin, vinylchloride, derived ellipticine derived taxane derived wortmannin and derived pyrazolopyrimidine.

30. The composition according to item 22, wherein therapeutic agent is selected from the group including doxorubicin, daunorubicin, mitomycin C, epirubicin, pirarubicin, ripidolite, carcinomain, N-acetylcarnitine, rubiazo, 5-imitational, N-azetidinol, daunomycin, mitoxantrone, camptothecin, 9-aminocamptothecin, 7-Etiketten, 10-hydroxycamptothecin, 9-nitrocamptothecin, 10,11-methylenedioxyamphetamine, 9-amino-10,11-methylenedioxyamphetamine, 9-chloro-10,11-methylenedioxyamphetamine, irinotecan, topo is a perfect combination, lurtotecan, silation, (7-(4-methylpiperazine)-10,11-Ethylenedioxy-20(S)-camptothecin, 7-(4-methylpiperazine)-10,11-methylenedioxy-20(S)-camptothecin, 7-(2-N-isopropylamino)ethyl)-(20S)-camptothecin, vincristine, vinblastine, vinorelbine, vinflunine, Vinpocetine, vindesine, ellipticine, 6-3-aminopropyl-ellipticine, 2-diethylaminoethyl-ellipticine and their salts, dateoption, reality, paclitaxel and docetaxel.

31. The composition according to item 22, wherein therapeutic agent is selected from the group comprising: antihistaminew derivative of Ethylenediamine, brompheniramine, diphenhydramine, Antiprotozoal medicine, hinolan, iodophenol, derived amidine, pentamidine, anthelmintic compound, Pyrantel, antihistamine medicine, examinedin, antifungal triazole derivative, fluconazole, Itraconazole, ketoconazole, miconazole, antimicrobial cephalosporins, Cefazolin, cefonicid, Cefotaxime, ceftazidim, ceoxime, antimicrobial beta-lactam derivative, aztreonam, cefmetazole, cefoxitin, antimicrobial agent from a group of erythromycin, erythromycin, azithromycin, clarithromycin, oleandomitsin, a derivative of penicillin, benzylpenicillin, phenoxymethylpenicillin, cloxacillin, methicillin, nafcillin, oxacillin, carbenicillin, a derivative of tetracycline, novobiocin, spectinomycin, vancomycin, antimycobacterial the medicine, aminosalicylic acid, capreomycin, ethambutol, isoniazid, pyrazinamide, rifabutin, rifampin, clofazimine, antivirus adamantane derivative, amantadine, rimantadine, a derivative of quinidine, quinine, hengren, chloroquine, hydroxychloroquine, primaquine, amodiaquine, mefloquine, an anti-microbial hinolan, ciprofloxacin, enoxacin, lomefloxacin, nalidixic acid, norfloxacin, ofloxacin, sulfonamide, antimicrobial agent for a urinary system, nitrofurantoin, trimethoprim, nitroimidazole derived, metronidazole, cholinergic derived Quaternary ammonium, amminium, neostigmine, physostigmine, aminoacridine as a tool against Alzheimer's disease, taken, medicine to treat Parkinson's disease, benztropine, biperiden, procyclidine, trihexyphenidyl, antimuskarinovoe act occurs, the agent, atropine, hyoscyamine, scopolamine, propantheline, adrenergic connection, dopamine, serotonin, albuterol, dobutamine, ephedrine, epinephrine, norepinephrine, isoproterenol, metaproterenol, salmeterol, terbutaline, an inhibitor of reagowania serotonin, a derivative of ergotamine, muscle relaxant family of curare, a muscle relaxant General action, baclofen, cyclobenzaprine, dantrolene, the nicotine receptor antagonist of nicotine, beta - blocker, Acebuchal, amiodarone, a derivative of benzodiazepine, ditiazem, an antiarrhythmic drug, d is isoperated, Engadin, the connection to the local anesthetic, procaine, procainamide, lidocaine, flecainide, quinidine, ACE inhibitor, captopril, enalaprilat, fosinopril, inapril, ramipril, opiate derivative, codeine, meperidine, methadone, morphine, antilipidemics agent, fluvastatin, gemfibrozil, HMG - CoA inhibitor, pravastatin, anti-hypertensive drug clonidine, guanabenz, prazosin, guanethidine, guanadrel, hydralazine, coronary and non-coronary vasodilator dipyridamole, an inhibitor of acetylcholinesterase, pilocarpine, the alkaloid physostigmine and neostigmine.

32. The composition according to item 22, wherein at least 90% of these substances remains encapsulated in the liposome through 6 months at 2-8°C.

33. The composition according to item 22, wherein at least 80% of these substances remains encapsulated in the liposome after 2 years at 2-8°C.

34. The composition according to item 22, wherein the said substance encapsulated in the liposomes of the composition when the first ratio of the substance/lipid and 24 h after injection of the composition into the blood stream of the mammal specified substance, agent or marker remain encapsulated in the liposomes at the second value of the substance/lipid, which is over 50%, at least 60% or at least 70% from the first ratio of the substance/lipid.

35. The composition according to clause 34, wherein the link is on is vinylchlorid.

36. The composition according to clause 34, wherein the specified substance is vinorelbine.

37. The composition according to clause 34, wherein the mammal is a rat.

38. The composition according to p, characterized in that it contains antineoplastics therapeutic agent encapsulated in it when the molar ratio of agent/lipid, approximately equal to 0.10, and liposomal composition has an in vivo antineoplastic activity at least four times higher than antineoplastics active agent in a free, liposomally form and toxicity of liposomal composition, introduced mammals, equal to or less than the toxicity of the agent administered to the mammal, in a free, liposomal form.

39. The composition according to § 38, characterized in that the toxicity of liposomal composition introduced to the mammal at least two times smaller or at least three times less than the toxicity of the specified composition is introduced to the mammal in a free, liposomal form.

40. The composition according to § 38, characterized in that the toxicity of liposomal composition introduced to the mammal at least four times lower than the toxicity of the specified composition is introduced to the mammal in a free, liposomal form.

41. The composition according to § 38, wherein the agent is an inhibitor of Cam is Tatarin-topoisomerase I.

42. The composition according to paragraph 41, characterized in that said inhibitor is irinotecan.

43. The composition according to paragraph 41, characterized in that the inhibitor is injected into the bloodstream of a mammal, characterized by the half-life of liposomes, at least 10 hours

44. The composition according to paragraph 41, characterized in that the inhibitor is injected into the bloodstream of a mammal, characterized by the half-life of liposomes, at least 24 hours

45. The composition according to paragraph 41, wherein the liposome comprises prinivilbuy disaccharide, which is polysulfonamide sucrose having from 3 to 8 of sulfate groups in the molecule.

46. The composition according to item 45, wherein poliuretonovaya sucrose is sharepointserver.

47. The composition according to item 13, wherein the liposome containing substituted ammonium having the formula
R₁-(R_2-)N⁺(R₃)-R₄
where N represents an ammonium nitrogen atom, each of R₁, R₂, R₃, R₄represents independently a hydrogen atom or an organic group having each independently not more than 8 carbon atoms and in General (in the aggregate) not more than 18 carbon atoms, inclusive, and at least one of R₁, R₂, R₃, R₄is an organic group, the organic group is and independently represents alkyl, alkyliden, heterocyclic alkyl, cycloalkyl, aryl, alkenyl, cycloalkenyl or replacement derivative, optionally containing atoms S, O or N, form an ether, ester, thioester, amino or amide bond, and
where at least three of R₁, R₂, R₃, R₄are organic groups, or at least one of the organic groups is a secondary or tertiary carbon atom directly linked to the ammonium nitrogen atom.

48. Composition according to any one of p or 42, wherein the topoisomerase inhibitor is captured in the liposome at a concentration of about 0.30 moles of drug per mole of lipid.

49. Composition according to any one of p or 42, wherein the topoisomerase inhibitor is captured in the liposome at a concentration of from about 0.40 mole of drug per mole of lipid to about 1.7 moles of drug per mole of lipid.

50. Composition according to any one of p-40 or 43, 44, characterized in that the mammal is a mouse.

51. Composition according to any one of p-46 or 48 to 50, wherein the antitumor activity determined in vivo in HT-29 tumor models or BT-474 tumor model.

52. The composition according to p-44, characterized in that the mammal is a rat.

53. The composition according to claim 1 or 13, intended for the introduction of vinylchloride medications, is great for the rpm die, that includes vinyltoluene medication when you first ratio of drug/liposome, characterized by the fact that after 24 h after injection of the composition into the blood stream of the mammal vinyltoluene medicine remains included in the liposomes when the second value is the ratio of drug/lipid that is greater than about 50% from the first ratio drug/lipid.

54. The composition according to item 53, wherein the second ratio of drug/lipid is about 60% from the first ratio drug/lipid.

55. The composition according to item 53, wherein the second ratio of drug/lipid is about 70% from the first ratio drug/lipid.

56. The composition according to p-55, characterized in that the first molar ratio of drug/lipid is at least of 0.05, at least 0.1 or at least 0,2.

57. The composition according to p, characterized in that the first ratio by weight of the drug/lipid is at least about 0.05 mg/mmol at least about 0.1 mg/mmol or at least about 0.3 mg/mmol.

58. Composition according to any one of p-57, characterized in that the liposomes comprise a transmembrane gradient of the ions in the direction of "inside/outside", which is able to retain the drug within liposomes.

59. Composition according to any one of p-58, characterized in that the inner space of the ash is separated prinivilbuy monosaccharide or prinivilbuy disaccharide.

60. Composition according to any one of p or 59, characterized in that the internal space contains ion or ammonium ion, substituted ammonium.

61. The composition according to p, characterized in that the ion substituted ammonium is an ion primary ammonium, secondary ammonium, tertiary ammonium or Quaternary ammonium.

62. Composition according to any one of p or 59, characterized in that the internal space contains ion substituted ammonium having the formula
R₁-(R_2-)N⁺(R₃)-R₄
where N represents an ammonium nitrogen atom, each of R₁, R₂, R₃, R₄represents independently a hydrogen atom or an organic group having each independently not more than 8 carbon atoms and in General (in the aggregate) not more than 18 carbon atoms, inclusive, and at least one of R₁, R₂, R₃, R₄is an organic group, the organic group independently represents an alkyl, alkylidene, heterocyclic alkyl, cycloalkyl, aryl, alkenyl, cycloalkenyl or replacement derivative, optionally containing atoms S, O or N, form an ether, ester, thioester, amino or amide bond, and where at least three of R₁, R₂, R₃, R₄are organic groups, or at least one organ of the economic group is secondary or tertiary carbon atom, directly related to the ammonium nitrogen atom, and where the specified internal space also includes anion.

63. The composition according to p, characterized in that prinivilbuy monosaccharide or prinivilbuy disaccharide is contained in the inner space at a concentration of at least 0.05 gram equivalent/l, at least 0.2 gram equivalent/l, at least 0.5 gram equivalent/l, at least 0.6 gram equivalent/L.

64. Composition according to any one of p-63, characterized in that vinyltoluene medicine is winprinter, vinblastine, vinorelbine, vinflunine, vindesine or Vinpocetine.

65. Composition according to any one of p-57, characterized in that the lipid is a phosphatidylcholine or cholesterol.

66. The composition according to p, wherein the phosphatidylcholine is selected from the group comprising natural lecithin, hydrogenomonas natural lecithin, synthetic lecithin, 1,2-distearoyl-lecithin, 1,2-dipalmitoyl-lecithin, 1,2-dimyristoyl-lecithin, 1,2-dioleoyl-lecithin, 1-stearoyl-2-oleyl-lecithin and 1-Palmitoyl-2-oleyl-lecithin.

67. The composition according to p, wherein the phosphatidylcholine and cholesterol are contained at a molar ratio of about 3:2.

68. The composition according to item 53, wherein the lipids are neutral PEG-derived lipid or anionic PEG-about svodnoe lipid.

69. The composition according to p, characterized in that the neutral PEG-derived lipid is from about 0.1 mol.% up to about 10 mol.% of the total number of lipids.

70. The composition according to p, characterized in that the neutral PEG-derived lipid is a PEG-ceramide, or PEG-diacylglycerol.

71. The composition according to p, characterized in that the anionic PEG-derived lipid contained in an amount less than 1 mol.% of the total number of lipids.

72. The composition according to p, characterized in that the anionic PEG-derived lipid represents -(ED)-dieselpartikelfilter.

73. The composition according to item 53, wherein the mammal is a rat.

74. The composition according to claim 1 or 13, intended for the introduction of vinylchloride drugs, including liposomes in an environment that has an internal space and a membrane separating the inner space from the environment and includes one or more lipids, and lipids are lecithin and cholesterol in a molar ratio of about 3:2, vinyltoluene the medicine contained in the liposomes at a ratio of drug/lipid from about 0.15 mg/mmol of lecithin to about 0.55 mg/mmol of lecithin, the internal space also contains prinivilbuy monosaccharide or prinivilbuy disaccharide, which is contained in the inner space of the liposomes at a concentration of orokolo 0.5 gram equivalent/L. up to about 1.0 gram equivalent/l, and vinyltoluene medicine is a vinorelbine, winprinter or vinblastine.

75. The composition according to p, characterized in that prinivilbuy disaccharide is sharepointserver.

76. The composition according to item 75, further comprising a neutral derivative of poly(ethylene glycol)-lipid in an amount of from about 0.1 mol.% up to about 10 mol.% of the total lipid.

77. The composition according to p, characterized in that a derivative of poly(ethylene glycol)-lipid is a poly(ethylene glycol)-dialkylglycerol, poly(ethylene glycol)-diacylglycerol or poly(ethylene glycol)-ceramide, and molecular weight poly(ethylene glycol)-specific poly(ethylene glycol)lipid a derivative is from about 250 to about 10,000.

78. The composition according to item 75, further comprising anionic derivative of poly(ethylene glycol)-lipid in an amount of from about 0.1 mol.% to about 0.9 mol.% of the total lipid.

79. The composition according to p, characterized in that the anionic derivative of poly(ethylene glycol)lipid is a PEG-phosphatidylethanolamine, and molecular weight poly(ethylene glycol)lipid a derivative is from about 250 to about 10,000.

80. Composition according to any one of p-79, characterized in that the half-life of the specified vinylchloride drugs from liposomes in the bloodstream mlekopitayushchie is about is more than 24 hours

81. The composition according to item 80, wherein the mammal is a rat.

82. The composition according to item 22, wherein incorporating therapeutic agent is Texan, which is contained mainly in the inner space of the liposome.

83. The composition according to p, characterized in that taxon is a neutral ion in relation to the substance.

84. The composition according to p, characterized in that the molecular structure taxane does not include the balance of the hydrophilic polymer.

85. Composition according to any one of p-84, characterized in that the amount of encapsulated taxane is at least 0.05 mole per mole of lipid.

86. The composition according to p, characterized in that the amount of encapsulated taxane is at least 0.1 mol to
mol lipid.

87. Composition according to any one of p-86, characterized in that the inner space largely free from solubilizing means selected from the micelle-forming surfactant and cyclodextrin.

88. The composition according to p, characterized in that taxon is a paclitaxel or docetaxel.

89. The composition according to any one of claims 1, 13, characterized in that the lipids include lipid a derivative is a product of the interaction of lipid with a hydrophilic polymer.

90. The composition according to p, characterized in that the content of the criminal code is related lipid derivative - the product of the interaction of lipid with hydrophilic polymer - up to 20 mol.% from the total lipid content.

91. The composition according to p, characterized in that the contents of the specified lipid derivative of the product of the interaction of lipid with hydrophilic polymer is less than 1 mol.% from the total lipid content.

92. The composition according to p, wherein the liposome has a durability circulation in the blood of a mammal in 2 times higher than the durability circulation liposomes identical composition but not containing the above-mentioned lipid derivative of the hydrophilic polymer.

93. The composition according to p, wherein the mammal is a rat.

94. The composition according to p, wherein the lipid derivative of the hydrophilic polymer is contained in an amount of from about 0.1 mol.% to about 0.9 mol.% from the total lipid content.

95. The composition according to p, characterized in that the hydrophilic polymer is a poly(ethylene glycol) or its derivative.

96. The composition according to p, wherein the lipid derivative of the hydrophilic polymer is a poly(etilenglikole) derived phospholipid, poly(etilenglikole) derived diacylglycerol, poly(etilenglikole) derived diacylglyceride, poly(etilenglikole) derived tzera the IDA, poly(etilenglikole) derived fatty acids, poly(etilenglikole) derived fatty alcohol or poly(etilenglikole) derived Sterol.

97. The composition according to p, characterized in that the hydrophilic polymer is a poly(ethylene glycol)having at least three etilenglikolevye units.

98. The composition according to p, characterized in that the hydrophilic polymer is a poly(ethylene glycol) with a molecular weight of from about 200 to about 10,000.

99. The composition according to p, characterized in that the hydrophilic polymer is a poly(ethylene glycol) with a molecular weight of from about 500 to about 5000.

100. The composition according to any one of claims 1, 13, characterized in that the liposome includes a guiding part.

101. The composition according to item 100, wherein the target part is a protein, peptide, polysaccharide, polynucleotide, natural substance is small, synthetic substance is small, a combination thereof or a derivative thereof.

102. The composition according to item 100, wherein the target part is a natural, synthetic or recombinant obtained by protein comprising the antigen-binding sequence of the antibody.

103. The composition according to item 100, wherein the target portion is an antibody, its antigen-binding FR is gment, single-chain protein comprising the antigen-binding polypeptide sequence of the antibody or single domain antibody.

104. The composition according to item 100, wherein the guiding part is connected with the membrane of the liposome and facing towards the environment.

105. The composition according to p, characterized in that the associated guiding part includes a hydrophilic polymer that binds to the membrane of the liposomes with this guiding part.

106. The composition according to p, characterized in that the hydrophilic polymer is a poly(ethylene glycol).

107. The composition according to p, wherein the poly(ethylene glycol) has a molecular weight from about 250 to about 30,000.

108. The composition according to p, characterized in that the guiding part performs the internalization of the liposome into the cell.

109. The composition according to p, wherein the target portion selectively binds to the receptor tyrosine kinase, growth factor receptor, a receptor for an angiogenic factor, transferrin receptor, adhesive substance cells or receptor vitamin.

110. The composition according to p, wherein the tyrosine kinase receptor is a growth factor receptor.

111. The composition according to p, characterized in that the receptor tyrosinekinase growth factor is EGFR, ErbB-2(HER2), ErbB-3(HER3,), ErbB-4(HER4).

112. The composition according to p, characterized in that Thu is the receptor for an angiogenic factor is a bFGF-receptor or VEGF-receptor.

113. The composition according to p, characterized in that the adhesive substance of the cell is an integrin.

114. Composition according to any one of p-113, characterized in that the cell is a malignant cell.

115. Method encapsulate substances in a liposome, comprising a stage of contacting the composition according to any one of claims 1 to 22 with a substance for a time sufficient to ensure that the specified substance was encapsulated in the liposome.

116. The method according to p, characterized in that at least part of the substance gets into the inner space of the liposome.

117. The method according to p, characterized in that at least 90% of the substance gets into the inner space of the liposome.

118. The method according to p, characterized in that the part of the substance, which becomes encapsulated in the liposomes is at least 80%, at least 90% or at least 95%.

119. The method according to p, characterized in that the substance is completely cationic substance, a therapeutic agent or detektivami token.

120. The method according to p, characterized in that the molar ratio of the specified substance to the total content of lipids is about 0.05, about 0.1, about 0.2, or about 0.3.

121. The method according to p, wherein therapeutic agent is an antimicrobial therapeutic agent, an antiviral terap whiteskin agent or antineoplastics therapeutic agent.

122. The method according to p, wherein therapeutic agent is an aminoglycoside antibiotic or a derivative fluoroquinolone.

123. The method according to p, wherein therapeutic agent is selected from the group comprising: a topoisomerase inhibitor, an inhibitor farnesyltransferase, a tyrosine kinase inhibitor, an inhibitor of cyclin-dependent kinase, a phosphatase inhibitor, inhibitor euroracing, microcalorimetry agent, microtubuleassociated agent, an alkylating agent, an enzyme, an enzyme inhibitor, an inhibitor of histone-deacetylase, an antimetabolite, a receptor-binding agent, a hormone, a hormone antagonist, nucleotide and polynucleotide.

124. The method according to p, characterized in that antineoplastics therapeutic agent selected from the group including derivative anthracycline, derived camptothecin, vinylchloride, derived ellipticine derived taxane derived wortmannin and derived pyrazolopyrimidine.

125. The method according to p, wherein therapeutic agent is selected from the group including doxorubicin, daunorubicin, mitomycin C, epirubicin, pirarubicin, ripidolite, carcinomain, N-acetylcarnitine, rubiazo, 5-imitational, N-azetidinol, daunomycin, mitoxantrone, camptothecin, 9-aminocamptothecin, 7-Etiketten, 10-hydroxycamptothecin, 9-nitrocatechol the Qing, 10,11-methylenedioxyamphetamine, 9-amino-10,11-methylenedioxyamphetamine, 9-chloro-10,11-methylenedioxyamphetamine, irinotecan, topotecan, lurtotecan, silation, (7-(4-methylpiperazine)-10,11-Ethylenedioxy-20(S)-camptothecin, 7-(4-methylpiperazine)-10,11-methylenedioxy-20(S)-camptothecin, 7-(2-N-isopropylamino)ethyl)-(20S)-camptothecin, vincristine, vinblastine, vinorelbine, vinflunine, Vinpocetine, vindesine, ellipticine, 6-3-aminopropyl-ellipticine, 2-diethylaminoethyl-ellipticine and their salts, dateoption, reality, paclitaxel and docetaxel.

126. The method according to p, wherein therapeutic agent is selected from the group comprising: antihistaminew derivative of Ethylenediamine, brompheniramine, diphenhydramine, Antiprotozoal medicine, hinolan, iodophenol, derived amidine, pentamidine, anthelmintic compound, Pyrantel, antihistamine medicine, examinedin, antifungal triazole derivative, fluconazole, Itraconazole, ketoconazole, miconazole, antimicrobial cephalosporins, Cefazolin, cefonicid, Cefotaxime, ceftazidim, ceoxime, antimicrobial beta-lactam derivative, aztreonam, cefmetazole, cefoxitin, antimicrobial agent from a group of erythromycin, erythromycin, azithromycin, clarithromycin, oleandomitsin, a derivative of penicillin, benzylpenicillin, phenoxymethylpenicillin, cloxacillin, methicillin, NAF is Illin, oxacillin, carbenicillin, a derivative of tetracycline, novobiocin, spectinomycin, vancomycin, antimycobacterial medicine, aminosalicylic acid, capreomycin, ethambutol, isoniazid, pyrazinamide, rifabutin, rifampin, clofazimine, antivirus adamantane derivative, amantadine, rimantadine, a derivative of quinidine, quinine, hengren, chloroquine, hydroxychloroquine, primaquine, amodiaquine, mefloquine, an anti-microbial hinolan, ciprofloxacin, enoxacin, lomefloxacin, nalidixic acid, norfloxacin, ofloxacin, sulfonamide, antimicrobial agent for a urinary system, nitrofurantoin, trimethoprim, nitroimidazole derived, metronidazole, cholinergic derived Quaternary ammonium, amminium, neostigmine, physostigmine, lipoamide as a tool against Alzheimer's disease, taken, medicine to treat Parkinson's disease, benztropine, biperiden, procyclidine, trihexyphenidyl, antimuskarinovoe act occurs, the agent, atropine, hyoscyamine, scopolamine, propantheline, adrenergic connection, dopamine, serotonin, albuterol, dobutamine, ephedrine, epinephrine, norepinephrine, isoproterenol, metaproterenol, salmeterol, terbutaline, an inhibitor of reagowania serotonin, a derivative of ergotamine, muscle relaxant family of curare, a muscle relaxant General action, baclofen, cyclobenzaprine, dantrolene, nicotine receptor antag nista nicotine, beta-blocker, Acebuchal, amiodarone, a derivative of benzodiazepine, ditiazem, antiarrhythmic medication, disopyramide, Engadin, the connection to the local anesthetic, procaine, procainamide, lidocaine, flecainide, quinidine, ACE inhibitor, captopril, enalaprilat, fosinopril, inapril, ramipril, opiate derivative, codeine, meperidine, methadone, morphine, antilipidemics agent, fluvastatin, gemfibrozil, HMG - CoA inhibitor, pravastatin, anti-hypertensive drug clonidine, guanabenz, prazosin, guanethidine, guanadrel, hydralazine, coronary and non-coronary vasodilator dipyridamole, an inhibitor of acetylcholinesterase, pilocarpine, alkaloid, physostigmine and neostigmine.

127. The method according to p-126, wherein the contacting is carried out in aqueous solution,

128. The method according to p, characterized in that the aqueous solution has a pH from about 4 to about 7.

129. The method according to p, characterized in that the aqueous solution has an ionic strength equivalent to or less than 50 mm of sodium chloride.

130. The method according to p, characterized in that the aqueous solution has an ionic strength equivalent to or less than 20 mm of sodium chloride.

131. The method according to p, characterized in that the aqueous solution has a pH between about 6.0 or around 7.0, and the substance is vinylchlorid.

132. The method according to p, characterized in that the pH of the aqueous solution is about 6.5, and ve is estvo is vinorelbine.

133. The method according to p, characterized in that the pH of the aqueous solution is between about 5 and about 7, and the substance is a derivative of camptothecin.

134. The method according to p, characterized in that the pH of the aqueous solution is between about 5 and about 6.5, and the substance is Topotecan or Irinotecan.

135. The method according to p or 130, wherein after said contacting the ionic strength of the aqueous solution increases, exceeding the ionic strength of 50 mm sodium chloride.

136. The method according to p, characterized in that the magnitude of the ionic strength increases, at least up to the value of the ionic strength of 100 mm sodium chloride.

137. The method according to p, characterized in that the magnitude of the ionic strength increases, at least up to values of ionic strength 150 mm sodium chloride.

138. The method according to any of PP-137, wherein the composition that comes into contact with the substance comprises a liposome and the liposome comprises a compound substituted ammonium having in aqueous solution at room temperature, the pKa value equal to at least 8.0 for at least an 8.5, at least, 9,0, at least 9.5 or at least, 10,0.

139. Set to provide liposomal encapsulated substances, including composition according to any one of claims 1 to 22 and not necessarily in a separate container the substance itself.

140. Set p, characterized in that the substance which is completely cationic substance, therapeutic agent or detektivami token.

141. The composition according to any one of claims 1, 13, characterized in that the liposome comprises a compound substituted ammonium having in aqueous solution at room temperature, the pKa value equal to at least 8.0 for at least an 8.5, at least, 9,0, at least 9.5 or, at least, and 10.0.