# US 2015/0148428 A1 · Micelle structure of nano preparation for diagnosis or treatment of cancer disease and preparation method thereof > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2015/0148428 A1 - Document ID: US20150148428A1 - Status: Published application - Kind: A1 - Application number: 14/315,943 - Filed: 2014-06-26 - Published: 2015-05-28 - Earliest claimed: 2013-11-22 - Assignees: Korea Advanced Institute of Science and Technology - Applicants: Korea Advanced Institute of Science and Technology - Inventors: Chulhee Choi; Kyuha Chong; Jiho Park - Web page: https://patentgrep.com/patent/US20150148428A1 ## CPC - A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids - A61K 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)} - A61K 31/122: having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin - A61P 35/00: Antineoplastic agents - 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) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract Disclosed herein are a nanopreparation having a micelle structure for diagnosis or treatment of cancer diseases, and a method of preparing the same, and more particularly, a nanopreparation having a micelle structure available for diagonosis or treatment of cancer diseases and a method for preparing the same, wherein the nanopreparation is prepared by encapsulating a photosensitizer by forming micelle with polymeric lipid DSPE-mPEG. The nanopreparation having the micelle structure according to the present invention has a size of 12 nm or less by encapsulating hypericin, which is a photosensitizer, by forming micelle with polymeric lipid DSPE-mPEG having a molecular weight of 1500 to 2500. Resultingly, the nanopreparation easily overcomes a blood-tumor barrier (BTB) and an interstitial fluid pressure and has light induced cytotoxicity efficiency that is about more than 2.5 times higher than that of the case where hypericin is used alone. ## Claims ### Claim 1 A nanopreparation having a micelle structure for diagnosis or treatment of cancer diseases, the nanopreparation comprising: 1.0 molar ratio of a photosensitizer; and 5.0 to 15.0 molar ratios of polymeric lipid DSPE-mPEG. ### Claim 2 (depends on 1) The nanopreparation as set forth in claim 1, wherein the photosensitizer is hypericin. ### Claim 3 (depends on 1) The nanopreparation as set forth in claim 1, wherein the DSPE-mPEG has a molecular weight of 1500 to 2500. ### Claim 4 (depends on 1) The nanopreparation as set forth in claim 1, wherein the nanopreparation has a size of 5.0 to 12.0 nm. ### Claim 5 (depends on 1) The nanopreparation as set forth in claim 1, wherein the nanopreparation is accumulated in a mitochondrion among intracellular organelles. ### Claim 6 (depends on 1) The nanopreparation as set forth in claim 1, wherein the cancer disease is selected from the group consisting of colon cancer, liver cancer, gastric cancer, breast cancer, colorectal cancer, bone tumor and cancer, pancreatic cancer, head and neck tumors or cancers, uterine cancer, ovarian cancer, rectal cancer, esophageal cancer, small intestine cancer, perianal cancer, colorectal cancer, fallopian tube carcinoma, endometrial carcinoma, cervical carcinoma, vagina carcinoma, vulva carcinoma, Hodgkin's disease, prostate cancer, bladder cancer, renal cancer, ureter cancer, renal cell carcinoma, renal pelvis carcinoma, central nervous system tumors and cancers, and brain tumors. ### Claim 7 (depends on 6) The nanopreparation as set forth in claim 6, wherein the brain tumor is selected from the group consisting of a pituitary tumor, meningioma, medulloblastoma, schwannoma, glioma, high-grade astrocytoma, glioblastoma, metastatic brain tumors, and other primary brain tumors. ### Claim 8 (depends on 1) A method of preparing the nanopreparation having the micelle structure of claim 1, the method comprising: mixing a photosensitizer and polymeric lipid DSPE-mPEG dissolved in an organic solvent at a molar ratio of 1.0:5.0 to 15.0 to prepare a mixed solution (step 1); removing the organic solvent from the mixed solution prepared in the step 1 and drying the resultant to prepare a polymeric lipid film (step 2); hydrating the polymeric lipid film prepared in the step 2 in one or more solutions selected from the group consisting of water, PBS, HBS, and HBG at room temperature to 100° C. to form nanoparticles having a micelle structure (step 3); and filtering the nanoparticles having the micelle structure formed in the step 3 to homogenize (step 4). ### Claim 9 (depends on 8) The method as set forth in claim 8, wherein the organic solvent of the step 1 is one or more solvents selected from the group consisting of chloroform, dimethyl sulfoxide, dimethylformamide, ethanol, methanol, tetrahydrofuran, toluene, xylene, and hexane. ### Claim 10 (depends on 8) The method as set forth in claim 8, wherein the polymeric lipid DSPE-mPEG of the step 1 has a molecular weight of 1500 to 2500. ### Claim 11 (depends on 8) The method as set forth in claim 8, wherein the photosensitizer is hypericin. ### Claim 12 (depends on 8) The method as set forth in claim 8, wherein the hydrating in the step 3 is performed in water and aging is then performed in one or more solutions selected from the group consisting of PBS, HBS, and HBG, or the hydrating is directly performed in one or more solutions selected from the group consisting of PBS, HBS, and HBG. ### Claim 13 (depends on 8) The method as set forth in claim 8, wherein the hydrating of the step 3 is simultaneously performed with sonication by a sonicator. ### Claim 14 (depends on 8) The method as set forth in claim 8, wherein the filtering of the step 4 is performed by a method including: filtering the nanoparticles having the micelle structure formed in the step 3 by a filter of 0.05 to 0.20 μm (step A); and re-filtering the nanoparticles filtered in the step A by a centrifugal filter of 20 to 40 K (step B).