# US 4,931,284 A · Micro-capsules > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 4,931,284 A - Document ID: US4931284A - Status: Granted - Kind: A - Application number: 07/074,700 - Filed: 1987-06-29 - Granted: 1990-06-05 - Earliest claimed: 1985-10-28 - Assignees: Biogram AB - Inventors: Bo M. Ekman; Kare V. Larsson; Ake R. Lindahl; Ulf S. E. Rothman - Web page: https://patentgrep.com/patent/US4931284A ## CPC - A61K 8/11: Encapsulated compositions - A61K 8/347: {Phenols} - A61K 8/375: {the alcohol moiety containing more than one hydroxy group} - A61K 9/1272: comprising non-phosphatidyl surfactants as bilayer-forming substances, e.g. cationic lipids or non-phosphatidyl liposomes coated or grafted with polymers (lipids as modifying agents {A61K47/543}) - A61K 9/1274: Non-vesicle bilayer structures, e.g. liquid crystals, tubules, cubic phases or cochleates; Sponge phases - A61Q 19/00: Preparations for care of the skin - B01J 13/08: Simple coacervation, i.e. addition of highly hydrophilic material {(combined with spraying B01J13/043; combined with mechanical division B01J13/04)} - A61K 2800/412: Microsized, i.e. having sizes between 0.1 and 100 microns - Y10T 428/2984: Microcapsule with fluid core [includes liposome] - Y10T 428/2989: Microcapsule with solid core [includes liposome] - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; 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; soap compositions C11D) - A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS - B01J: CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS - Y10T: TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION ## Abstract The invention relates to a completely novel type of micro-capsules, viz. such capsules where an encapsulated hydrophobic or lipophilic substance is surrounded by polar solid crystals of polar lipids which expose their hydrophilic face outwards and their hydrophobic face turned inwards towards the hydrophobic or lipophilic substance. These micro-capsules can be utilized to encapsulate for instance tacky substances or substances to be protected against oxidation or influence from light. Moreover, an especially interesting use according to the invention is the use of said micro-capsules in an ointment base, where the active ingredient is well protected within said capsules up to the use but which at the application on the skin directly comes into contact with the skin surface as a consequence of the crystalline structure of the shell. Furthermore, the invention relates to a special micro-capsule composition in the form of a dispersion of said micro-capsules in water or a polar liquid, where the crystals constitute 5-50 percent by weight and water or the polar liquid 50-95 percent by weight. Moreover, the invention relates to a process for the preparation of said micro-capsules, wherein a mixture of said polar lipid with water or polar liquid is formed, the mixture is heated above the transition temperature of the lipid and the mixture is then cooled to the desired temperature so as to obtain crystallization, the hydrophobic or lipophilic substance being added before or during the lipophilic phase. Finally, the invention relates to a crystal dispersion of the polar lipid in a polar liquid, such as glycerol, ethylene- or propylene glycol. ## Claims ### Claim 1 A micro-capsule composition consisting essentially of a hydrophobic or lipophilic substance surrounded by surface-active solid crystals of polar lipids, which crystals have a hydrophilic side that is exposed outwards and a hydrophobic side that is turned inwards toward the hydrophobic or lipophilic substance. ### Claim 2 (depends on 1) The micro-capsule composition of claim 1, wherein the lipid has a crystallization temperature of between about 20.degree. C. and about 100.degree. C. ### Claim 3 (depends on 1) The micro-capsule composition of claim 1, wherein the hydrophobic or lipophilic substance is coal-tar. ### Claim 4 (depends on 1) The micro-capsule composition of claim 1, wherein the hydrophobic or lipophilic substance is selected from the group consisting of marine oils, ditranol, vitamin A, vitamin D and flavonoides. ### Claim 5 (depends on 4) The micro-capsule composition of claim 4, wherein the flavonides are selected from the group consisting of catechin, rutin, rotenon, pyretrum and tannin. ### Claim 6 (depends on 1) The micro-capsule composition of claim 1 wherein the hydrophobic or lipophilic substance is tetracycline. ### Claim 7 (depends on 1) The micro-capsule composition of claim 1, wherein the hydrophobic or lipophilic substance constitutes greater than zero and up to about 90 percent by weight of the micro-capsule. ### Claim 8 (depends on 1) The micro-capsule composition of claim 1 consisting essentially of a dispersion of the micro-capsules in water or any other polar liquid having the ability of forming surface-active solid crystals from polar lipids, the polar liquid constituting from about 50 to 95 percent by weight of the dispersion, and the surface-active crystals constituting from about 5 to 50 percent by weight of the dispersion. ### Claim 9 (depends on 8) The micro-capsule composition of claim 8, wherein the micro-capsules are dispersed is water. ### Claim 10 (depends on 8) The micro-capsule composition of claim 8, wherein the proportion of hydrophobic or lipophilic substance is from about 0.1 to 15 percent by weight of the composition. ### Claim 11 (depends on 1) The micro-capsule composition of claim 1 in an ointment base. ### Claim 12 (depends on 1) The micro-capsule composition of claim 1, wherein the lipid crystals are .beta.-crystals of a lipid selected from the group consisting of monoglycerides of fatty acids, ascorbic acid esters of fatty acids, phosphate esters of fatty acids, lactic acid esters of fatty acids and monoglycerol ethers. ### Claim 13 (depends on 12) The micro-capsule composition of claim 12, wherein the fatty acids and the ether chains have 12 to 18 carbon atoms. ### Claim 14 (depends on 12) The micro-capsule composition of claim 12, wherein the monoglyceride is selected from the group consisting of 1-monolaurin, 1-monomyristin, 1-monopalmitin and 1-monostearin. ### Claim 15 (depends on 12) The micro-capsule composition of claim 12, wherein the monoglyceride is a mixture of two or more of the monoglycerides. ### Claim 16 (depends on 15) The micro-capsule composition of claim 15, wherein the mixture is 1-monolaurin and 1-monomyristin such that the proportion of 1-monolaurin is at least 10 percent by weight. ### Claim 17 (depends on 12) The micro-capsule composition of claim 12, wherein the fatty acids and the ether chains are saturated. ### Claim 18 A crystal dispersion of a polar lipid in a polar liquid other than water, wherein the dispersion consists essentially of a dispersion of the polar lipid in a polar liquid other than water and having the ability of forming polar solid crystals of the polar lipid where the polar liquid constitutes from about 50 to 95 percent by weight of the dispersion, and where the molecular orientation of the polar lipid within the crystal is such that the crystal surface consists essentially of polar end groups of the lipid, which impart hydrophilic properties to said crystals. ### Claim 19 (depends on 18) The crystal dispersion of claim 18, wherein the polar liquid is selected from the group consisting of glycerol, ethylene glycol and propylene glycol.