Liposomal nanocapsule

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of liposomal preparative form for medical-cosmetic and external pharmacologic application. Liposomal nanocapsule represents hollow sphere, formed by two-layer lipid coating, which contains external and internal hydrophilic layers, which include water extract of peloids, between which placed is hydrophobic area of two-layer lipid coating, which includes lipid extract of peloids, oppositely charged molecules of which are placed on surfaces of external and internal hydrophilic layers. Liposomal nanocapsule contains, %: water extract of peloids - 74%, lipid extract of peloids - 20%, vitamin E - 5%, stabiliser with phospholipid base- 1%.

EFFECT: invention ensures enhancement of medical-cosmetic effect of liposomal nanocapsule.

1 dwg, 1 tbl, 2 ex

 

The invention relates to the field of applied biotechnology, namely the liposomal structures preparative forms for health and beauty and outdoor pharmacological applications.

One of the types of nanocapsules include liposomes, which are containers for drug delivery. The membrane of liposomes composed of natural phospholipids, which determines their many attractive qualities. They are non-toxic, biodegrability, under certain conditions, can be absorbed by the cells, the membrane may merge with the cell membrane, which leads to intracellular delivery of their content.

A very important property of liposomes (as, indeed, and other nanoparticles) became the basis for the design of effective drugs. We are talking about the ratio of nanoparticle size and diameter of the pores of the capillaries. As the size of nanoparticles is larger than the diameter of the pores of the capillaries, their volume of distribution is limited to contrarotate introduction. For example, when intravenously, they do not extend beyond the blood flow, i.e. need badly to penetrate into tissues and organs. Therefore sharply reduced the toxic effect of the substance associated with nanoparticles. On the other hand, this property can serve as a basis for targeted delivery of chemotherapeutic drugs in inflammation and Defoe is prolonged, as the capillaries that supply these areas with blood, as a rule, heavily perforated. Therefore, the nanoparticles will accumulate in the inflammation and deformation. This phenomenon is called passive targeting. Thus, there are two reasons why liposomal drugs anti-inflammatory and regenerating substances are very effective: reducing toxicity and passive targeting.

Currently, the global pharmaceutical market has several liposomal preparations (Northfelt D.W., Kaplan L., Russell J. et al. (1995) in Stealth Liposomes (Lasic D.D., Martin F.J., eds). 257-266. CRC Press; Bogner J.R., Goebl F-D. (1995) in Stealth Liposomes (Lasic D.D., Martin F.J., eds). 267-278. CRC Press).

However, a disadvantage of the above analogues - liposomal drugs is the rapid elimination of liposomes from the blood, which is associated with the absorption of them by the reticuloendothelial system (RES) of the liver and spleen. This is due to the interaction of liposomes with plasma proteins - opsonins (mainly components of the complement). Opsonins "mark" liposomes, make them targets for cell RES.

A known design of liposomes phospholipids (RF patent No. 2270683, publ. 27.02.2006,), which sterically stabilized covalently linked dimetilformamidom and polyethylene glycol 2000.

The disadvantage of this liposome is that it's not the soda is incorporated drug and is intended only for aerosol injection into the body, not for injection.

Similar is also the liposomal nanocapsule form of a hollow sphere, formed by a lipid bilayer membrane of phosphatidylcholine and dimyristoylphosphatidylcholine containing internal and external hydrophilic lipid layers, between which there is a hydrophobic region of the bilayer lipid membrane. In addition, the nanocapsule contains drug doxorubicin, positively charged molecules which are located on the surfaces of the outer and inner hydrophilic lipid layers and attached to the negatively charged molecules of dimyristoylphosphatidylcholine (utility model RU 42953 U1, IPC A61K 9/127, publ. 27.12.2004,).

However, a disadvantage of the above liposomal nanocapsules is the specificity of action of the medicinal product doxorubicin and, therefore, a very narrow scope.

The closest technical solution (prototype) is a liposomal nanocapsule (PM No. 95519 from 10.07.2010), which is a hollow sphere formed bilayer lipid membrane containing an outer and inner hydrophilic layer, between which there is a hydrophobic region of the bilayer lipid membrane, polar charged molecules which are located on the surfaces of the outer and inner hydrophilic layer. ipina shell contains as internal and external hydrophilic layers of aqueous extract of peloids, and a hydrophobic region serves as a lipid extract of peloids.

However, these nanocapsules are characterized by insufficient medical cosmetic effect.

The technical result of the invention is the enhancement cosmetic effect.

This technical result is achieved by the fact that in the liposomal nanocapsule form of a hollow sphere, formed by a lipid bilayer membrane containing the external and internal hydrophilic layers, between which there is a hydrophobic region of the bilayer lipid membrane, polar charged molecules which are located on the surfaces of the outer and inner hydrophilic layer and double-layer lipid membrane contains as an external and internal hydrophilic layers of aqueous extract of peloids, and a hydrophobic region serves as a lipid extract of peloids, according to the claimed technical solution of the lipid membrane further comprises as a medical-cosmetic products vitamin E with the following content of all components of liposomal nanocapsules, %:

aqueous extract of peloids - 74;

the lipid extract of peloids - 20;

vitamin E - 5;

the stabilizer of a phospholipid basis - 1.

The invention is illustrated in the drawing, which shows the design of liposomal nanocapsules.

Lipase the material, the nanocapsule is a hollow sphere, formed by two-layer membrane containing 1 external and 2 internal hydrophilic layers on the basis of an aqueous extract of peloids, between which there is a hydrophobic region 3 two-layer membrane on the basis of the lipid extract of peloids containing a specified percentage of vitamin E (5%). Water and lipid extracts of peloids are pronounced therapeutic and cosmetic effect.

Examples of receiving liposomal nanocapsules

Example 1. Technology of production of liposomal nanocapsules with cosmetic biologically active substances

Water and oil extracts of peloids mixed together until a homogeneous emulsion and put pressure on the extruder sequentially through a membrane with a pore size of 1000, 800, 400, 200 and 100 nm several times through each membrane. Then the product is filtered through a filter with pore size of 220 nm for sterilization, pour it into bottles.

Example 2. Preparation of extracts and complexes on the basis of peloids

Use as a solvent two-phase system of solvents (alcohol-water mixture/oil) allows for one cycle to get water-alcohol and oil extraction, i.e. proektirovanii from raw materials hydrophilic and hydrophobic substances. Two-phase extraction based on preliminary wetting of raw materials 96% Adilov the m alcohol and extract it for 1.5-2 hours Then add the vegetable oil, purified water, bringing to a required concentration of alcohol-aqueous extractant and the ratio of the phases (raw materials/oil/alcohol-water mixture). The extraction is carried out at heating (80°C) and periodic stirring. Then divide by the density of the extract (alcohol-water and oil).

High efficiency two-phase extraction system of extractants in comparison with the extraction of oil is determined by the role of the alcohol phase (its composition and quantity) as a factor of swelling of vegetable raw materials, intermediate solvent and carrier of lipophilic substances from the cells of dry plant material in the oil phase. Upon contact of the feedstock with a liquid phase extractants alcohol-water mixture due to lower viscosity can easily penetrate into the plant material, desorption of naturally intracellular BAS and migrates by diffusion through the porous cell walls in the alcohol-water phase. Then the process of extraction liquid-liquid (alcohol-water solution - oil) under stirring with a stirrer. Between the alcohol-water and oil phases is a mass transfer process resulting in the redistribution of hydro - and lipophilic compounds between phases in accordance with the distribution coefficients. While predominantly hydrophilic substances remain in the alcohol-water phase and lipophilic PE ECODAT in oil. The output of this technology is 60-70%.

The results of the study of liposomal drug manifestation of local therapeutic effect

The objective of the stage of experimental research was the study of local and General biological effect when applied nanoliposomal capsules on the basis of extracts of peloids and vitamin E on the skin surface.

Conducted 20 series of experiments (6 control and 14 experienced) 276 outbred rats-males weighing 200-300, Rats were placed in individual cages and were observed for 27 days. Skin treatment was carried out daily, once daily, in the morning in 9 : 00 o'clock At the same time carried out as a General observation of animals (behaviors, General condition, appetite, sleep, natural origin), and the nature of the skin condition (appearance, character and rate of epithelialization, the presence and character of discharge). 2, 7, 14, 21, 27 days was conducted intake on biochemical, immunological, pathological studies.

Studies (see table) confirm the strengthening of the cosmetic effect compared to the prototype.

The content of neutral lipids in the surface lipid film of the skin, %
Index After application of liposomal nanocapsules without vitamin EAfter application of liposomal nanocapsules with vitamin E
FL11,21±1,2610,85±0,80
XC20,00±1,8121,07±0,76
LCDof 8.92±1,289,50±1,06
TAG20,50±1,94to 21.15±1,78
EHS39,14±3,0945,00±1,39
Note
PL - phospholipids; LDL - cholesterol; LCD fatty acids; TAG - triacylglyceride; EHS - esters of cholesterol

Thus, the use of this tool provides a positive dynamics of clinical and biochemical parameters of the blood system, as well as the health of the skin.

Liposomal nanocapsule form of a hollow sphere, formed by a lipid bilayer membrane containing the external and internal hydrophilic layers, between which there is a hydrophobic region of the bilayer lipid membrane, polar charged molecules which are located on the external surfaces and inside is it the hydrophilic layer, moreover, the lipid bilayer membrane contains as an external and internal hydrophilic layers of aqueous extract of peloids, and a hydrophobic region serves as a lipid extract of peloids, characterized in that the lipid membrane further comprises as a medical-cosmetic products vitamin E with the following content of all components of liposomal nanocapsules, %:

Aqueous extract of peloids74
The lipid extract of peloids20
Vitamin E5
The stabilizer of a phospholipid-based1



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics, and concerns a dosage form presented in the form of a capsule having a shell wall, a linker or another capsule subunit consisting of a pharmaceutically acceptable composition containing (i) ammonium methacrylate copolymer type A (Eudragit RL), (ii) at least one excipient modifying dissolution and presenting a hydroxypropyl cellulose polymer blend of various molecular weights and (iii) a lubricating agent.

EFFECT: invention provides polymer compositions applicable for melt extrusion and injection moulding, enabling time variations of shell dissolution and components release from the capsule.

32 cl, 12 ex

FIELD: medicine.

SUBSTANCE: invention refers to a liposomal preparative form for dermatological and external pharmacological application. A liposomal nanocapsule represents a hollow sphere formed by a bilayer lipid membrane containing inner and outer hydrophilic layers comprising an aqueous extract of peloids with a hydrophobic area of the bilayer lipid membrane in between, comprising a lipid extract of peloids and polar charged molecules being arranged on the surfaces of the inner and outer hydrophilic layers. The liposomal nanocapsule comprises: an aqueous extract of peloids - 64%, an lipid extract of peloids - 25%, an aqueous complex of humic acids - 10%, a phospholipid-based stabiliser - 1%.

EFFECT: invention provides enhanced therapeutic and cosmetic effect of the liposomal nanocapsule.

1 dwg, 1 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: declared invention refers to chemical-pharmaceutical industry, and concerns new, taste-masking powders specified in a group consisting of biologically active substances for treating, relieving and preventing diseases in humans and animals, with average particle diameter d50 1 to 40 mcm and coating thickness 1 to less than 20 mcm of a hydrophobic coating material containing 50 to 90 wt % (relative to total powdered solid substance and coating material) with the hydrophobic coating material being wax of fusion temperature within 30 to 180°C, resin, polymethacrylate or its copolymer for inhalation or oral administration.

EFFECT: what is offered is a simple method for preparing and applying them for introducing the biologically active substances.

10 cl, 3 ex

Microcapsules // 2359662

FIELD: medicine, pharmaceutics.

SUBSTANCE: microcapsules, in which water droplet or droplets including the dissolved active ingredient are incapsulated in the hardened hydrophobic cover-matrix, are described. Also the methods of obtaining of the specified microcapsules and their application are described.

EFFECT: development of microcapsules which possess the improved stability and provide the adjustable and-or prolonged release of an active ingredient.

40 cl, 8 dwg, 4 tbl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention claims pellet with enterosoluble shell, including ixabepilone with structure (A). Also a capsule containing multiple pellets with enterosoluble shell is claimed. Pellet includes particle with coating, containing main particle and active component layer distributed completely or partially on or in the main particle. Active component layer includes ixabepilone of structure (A) and binding agent. In addition, versions of obtaining pellet with enterosoluble shell are claimed.

EFFECT: reduced or prevented ixabepilone powder flaking, possible oral administration of ixabepilone without combined acid-neutralising buffer administration.

14 cl, 4 tbl, 3 ex

FIELD: medicine; pharmacology.

SUBSTANCE: invention refers to new composition of antifungal and fungicidal action, and applied for treatment of diseases caused by bacterial and fungal infection. Composition of prolonged action contains active substances antibacterial (chlorhexidine 0.02-0.05 mass%), antifungal (clotrimasole - 0.4-0.6 mass%), dimexide (7.0-27.0 mass%) as potentiator intensifying penetration of active substances, and also the stabiliser based on polyvinyl alcohol solution in physiologic saline, and structurally represents polymeric matrix with immobilised active components made as gel or a film from which active components are gradually released during application.

EFFECT: invention provides reduction of treatments time for ENT-diseases and dermal diseases of both candidal and mixed aetiology.

3 cl, 1 tbl

The invention relates to a metered composition of extended release within 24 h and a single dosage form of the composition in the form of capsules, including spheroids containing venlafaxine hydrochloride, microcrystalline cellulose and hypromellose

The invention relates to the field of medicine and veterinary medicine, namely to pharmacology, in particular, probiotics, and can be used in the correction of microbiocenosis of an organism of the person (adults and children) and animals

FIELD: medicine.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents nanoparticles containing a biodegradable polymer, cyclodextrin or their derivative and a biologically active molecule wherein said biodegradable polymer is a polyvinylmethylether maleic anhydride (PVM/MA) copolymer; and said biologically active molecule is a substance representing a substrate of P-glycoprotein enzyme.

EFFECT: invention provides higher bioavailability of lipophilic oral drugs or those being the substrate of P-glycoprotein enzyme.

9 cl, 7 ex, 9 tbl, 8 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry and represents pharmaceutical composition of prolonged action which includes non-agglomerated particles, containing active substance glycine and auxiliary substances, characterised by the fact that non-agglomerated particles represent nanoparticles with size from 170 to 500 nm, containing biodegradable polymer, as auxiliary substance polyvinyl alcohol as SAS, poloxamer as stabilising agent and cryoprotectant.

EFFECT: invention ensures increase of bioavailability of active substance glycine resulting from application in composition of biodegradable polymer, due to which coefficient of transmission and glycine assimilability increase, and time of glycine activity in organism grows.

4 cl, 5 ex

FIELD: medicine.

SUBSTANCE: invention refers to a liposomal preparative form for dermatological and external pharmacological application. A liposomal nanocapsule represents a hollow sphere formed by a bilayer lipid membrane containing inner and outer hydrophilic layers comprising an aqueous extract of peloids with a hydrophobic area of the bilayer lipid membrane in between, comprising a lipid extract of peloids and polar charged molecules being arranged on the surfaces of the inner and outer hydrophilic layers. The liposomal nanocapsule comprises: an aqueous extract of peloids - 64%, an lipid extract of peloids - 25%, an aqueous complex of humic acids - 10%, a phospholipid-based stabiliser - 1%.

EFFECT: invention provides enhanced therapeutic and cosmetic effect of the liposomal nanocapsule.

1 dwg, 1 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of pharmaceutics and deals with pharmaceutical compositions, which contain a) nanoparticles, containing poorly soluble in water pharmaceutical substance, for example taxane, and albumen; b) edetate and c) sucrose, where significant growth of microbes in composition is suppressed. Invention describes vial and set, which contain claimed compositions. In addition, claimed is application of composition for obtaining medications for treatment of cancer diseases, as well as method of treating cancer diseases. Invention also deals with method of conservating composition, which contains a) nanoparticles, containing poorly soluble in water pharmaceutical substance and albumen and b) sucrose, including addition of edetate into composition. Invention ensures reduction of undesirable oligomerisation of albumen, improved ability of slowing down microbial growth and faster restoration of lyophilised composition. In addition, in case, when as poorly soluble pharmaceutical substance applied is taxane, compositions demonstrate improved profile of.

EFFECT: invention ensures reduction of undesirable albumen oligomerisation, improved ability of slowing down microbial growth and faster restoration of lyophilised composition, in addition, in case, when as poorly soluble pharmaceutical substance applied is taxane, compositions demonstrate improved profile of absence of admixtures in taxane.

61 cl, 1 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: substance of the invention involves a stem cell (SC) preparation with reprogrammed cell signalling containing a base SC preparation in a membrane and/or a nucleus and/or a cytoplasm of which there is implanted a protein or pharmaceutical preparation capable to regulate signalling pathways of the SC and nidus cells in a mammal's body, pre-encapsulated in a nanocontainer with dimensions of 100 nm, produced of a biodegradable material, intact for organelles and compartments of the SC of the base preparation. This material has the preset biodegradation time in a mammal's body to provide the programmed protein or pharmaceutical preparation recovery in an intra- or intercellular space and to implement thereby reprogramming of signalling transduction of the SC key genes in a required therapeutic pattern of physiological cell cycle events directly in a pathological body region or tissue.

EFFECT: provided target addition of the signalling substances strictly in the involved body region.

14 cl, 6 ex, 3 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a composition of microparticles or nanoparticles for local delivery and delivery to a mucous surface of an active ingredient containing 0.1-99.5 wt % of an inorganic element chosen from alkaline, earth or transition metal, lanthanide or silicon dioxide, alkoxide, oxide, oxalate, ureate, nitrate or acetate, 0.01-95 wt % of a pharmaceutical or cosmetically active ingredient, and 0.001-75 wt % of a release control agent chosen from natural, synthetic or semisynthetic polymers, polysaccharides, monosaccharides, salts, fibres or peptides. Also, the invention covers methods for making said composition which involve dissolving each ingredient in a solvent, mixing the prepared solutions, adding a solution of alkaline hydroxide and producing a dry powder composition or gel colloidal solution of nanoparticles. Besides, the invention refers to a kit comprising said composition, a delivery device and an application data sheet.

EFFECT: invention provides better fixation in an effective area, effective absorption and controlled release.

34 cl, 9 tbl, 2 dwg, 6 ex

FIELD: medicine.

SUBSTANCE: invention concerns medicine, oncology, and can be used for selective destruction of tumours. For this purpose, a photosensitiser is encapsulated in polymeric microcontainers enclosed in shells that contain magnetite (Fe3O4) nanoparticles, and introduced in the surrounding biological tissue. The external constant magnetic field with its spatial configuration matched with the tumour shape is generated in the tumour bulk. Laser exposure follows within a given period corresponding to maximum accumulation of the microcontainers in the tumour at radiant energy density sufficient for photodynamic or photothermal destruction of the microcontainers shells in the tumour and following photodynamic or photothermal destruction of malignant cells. The photosensitiser is specified with an absorption band chosen with an absorption strip in red and close IR-spectral region 650-1200 nm.

EFFECT: method allows more effective destruction of cancer cells ensured by higher degree of photosensitiser accumulation in the tumour with minimal destruction of the surrounding healthy cells and a surgical procedure without general anaesthesia.

4 cl, 9 dwg

FIELD: medicine.

SUBSTANCE: invention discloses use of nanoparticles containing a matrix of at least one protein containing at least one anti-tumour active substance for preparing a medicinal agent for treating tumours whose resistance to chematherapeutic agents is associated with hyperexpression of P-glycoprotein, wherein the protein matrix includes at least one anti-tumour active substance which is not covalently bonded to said proteins.

EFFECT: doxorubicin nanoparticles in the disclosed medicinal agent and doxorubicin solution had comparable effect on non-resistant neuroblastoma cells; when resistance arose during therapy with cytostatic doxorubicin nanoparticles, the solution and liposomal preparation of doxorubicin were more effective in the disclosed agent.

4 cl, 2 dwg, 2 tbl

FIELD: medicine.

SUBSTANCE: invention refers to medicine and concerns nanoparticles containing vinyl methyl ether and maleic anhydride (PVM/MA) copolymer, or its derivatives.

EFFECT: present invention provides better bioadhesion, and as a consequence prolonged retention time in close contact with mucous membranes.

26 cl, 7 ex, 13 dwg, 10 tbl

FIELD: medicine.

SUBSTANCE: invention relates to food, pharmaceutical and cosmetic industry, in particular deals with oil-in-water emulsion, containing disperse oil drops which have nano-size self-arranging structured internal contents, including: (i) oil, (ii) lipophilic additive (LPA), (iii) hydrophilic domains in form of drops or small canals, containing water or non-water polar liquid, and continuous water phase, which contains emulsion stabilisers or emulsifiers, in which oil drops with diametre from 5 nm to 900 mcm possess nano-size self-arranging structuring with formation of hydrophilic domains with diametre from 0.5 to 200 nm due to presence of lipophilic additive.

EFFECT: invention provides structures able to solubilise not only lipophilic but at the same time hydrophilic and/or amphiphilic, or hydrotropic, or crystalline components.

8 cl, 16 ex, 18 dwg

FIELD: medicine.

SUBSTANCE: invention refers to pharmacology and represents a pharmaceutical composition for integrated treatment of ocular surface diseases in the patients suffering primary open-angle glaucoma, on the basis of phospholipids and sulphated glycosaminoglycans, differing by the fact that composition represents a liposomal emulsion formed by phospholipids in the form of liposomes, of average particle size 0.05-0.22 mcm, and sulphated glycosaminoglycans with sulphated glycosaminoglycans presented by keratan sulphate sodium salt and chondroitin sulphate sodium salt with the ingredients of the composition taken in certain proportions, wt %.

EFFECT: invention provides preventing lachrymal production from decreasing, reducing tear evaporation, as well as avoiding pathological changes in conjunctival and corneal epithelial cells.

5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to ophthalmology. A pharmaceutical composition is applicable in ophthalmology and contains the non-steroid anti-inflammatory drug indometacin and a phospholipid agent of the nanoparticle size 10-30 nm herbal phosphatidylcholine, maltose in the following proportions, wt %: phosphatidylcholine 20-43, maltose 55-78, indometacin 2-8. The indometacin and soya phospholipid composition represents a lyophilised powder.

EFFECT: invention provides prolonged storage stability of the composition.

2 dwg, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine and is applicable in the form of liposome-containing compounds for cancer therapy. A liposome contains one or more phosphatidylcholines, a first derivative of N-(ω)-dicarboxylic acid and phosphatidylethanolamine, an orientation modified derivative of N-(ω)-dicarboxylic acid and phosphatidylethanolamine, an encapsulated therapeutic agent and at least one additional lipid which represents cholesterol or a cholesterol derivative. The orientation modified derivative of N-(ω)-dicarboxylic acid and phosphatidylethanolamine contains an orientation ligand attached to a second derivative of N-(ω)-dicarboxylic acid and phosphatidylethanolamine. The first derivative of N-(ω)-dicarboxylic acid and phosphatidylethanolamine is presented by formula 1,

and the second derivative of N-(ω)-dicarboxylic acid and phosphatidylethanolamine is presented by formula 3, . The orientation ligand preferentially represents transferring, while the encapsulated therapeutic agent is oxalyplatine. The liposome is free from non-modified phosphatidylethanolamine, egg phosphatidylcholine or hydrophilic polymer used to prolong a half lifetime of the liposome in a circulatory channel, and the orientation ligand is other than an intact antibody. What is also described is a method of producing the liposome and a method of treating cancer with using it.

EFFECT: group of inventions provides better target delivery of the therapeutic substance in the tumour cells.

113 cl, 25 dwg, 4 tbl, 30 ex

Up!