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Osteoclast targeting delivery system based on small nucleic acid medicine and preparation method of osteoclast targeting delivery system

A technology of small nucleic acid drugs and osteoclasts, which is used in drug combinations, pharmaceutical formulations, gene therapy and other directions to achieve the effects of strong specificity, high affinity and easy absorption

Active Publication Date: 2016-10-05
BEIJING HELI CONSULTING CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, drug delivery systems that can specifically target osteoclasts have not been reported

Method used

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  • Osteoclast targeting delivery system based on small nucleic acid medicine and preparation method of osteoclast targeting delivery system
  • Osteoclast targeting delivery system based on small nucleic acid medicine and preparation method of osteoclast targeting delivery system
  • Osteoclast targeting delivery system based on small nucleic acid medicine and preparation method of osteoclast targeting delivery system

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Embodiment 1

[0049] An embodiment of the osteoclast targeted delivery system based on small nucleic acid drugs of the present invention, the osteoclast targeted delivery system based on small nucleic acid drugs in this embodiment includes liposomes and eight gates with thiol-modified ends Aspartic acid polypeptide repeat sequence ((D-Asp8)-SH) and the blocking agent miR-148a antagomir of microribonucleic acid; Wherein, liposome is made up of the lipid of following mass percentage: distearoylphosphatidylethanolamine- Polyethylene glycol 2000-maleimide (DSPE-PEG-MAL) 5%, 1,2-dioleyloxy-3-trimethylaminopropane (DOTAP) 15%, DC-cholesterol (DC-Chol) 50%, dioleoylphosphatidylethanolamine (DOPE) 15% and distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) 15%. In the targeted delivery system of this embodiment, the molar ratio of (D-Asp8)-SH to liposomes is 2: 100, and the mass ratio of microRNA blocking agent miR-148a antagomir to liposomes is 10%, The encapsulation effici...

Embodiment 2

[0056] An embodiment of the small nucleic acid drug-based osteoclast targeted delivery system of the present invention, the small nucleic acid drug-based osteoclast targeted delivery system in this embodiment includes liposomes and eight gates with thiol-modified ends Blocker of aspartic acid polypeptide repeat ((D-Asp8)-SH) and microRNA. Wherein, liposome is made up of the lipid of following mass percentage: dioleoyl dimethyl ammonium propane (DODAP) 10%, dioleoyl phosphatidylethanolamine (DOPE) 10%, distearoyl phosphatidyl choline (DSPC) ) 15%, DC-cholesterol (DC-Chol) 60% and distearoylphosphatidylethanolamine-polyethylene glycol 2000-maleimide (DSPE-PEG-MAL) 5%; microRNA blocking The agent is composed of miR-29a, miR-29b and miR-29c, and the mass percentages of miR-29a, miR-29b and miR-29c are 30%, 30% and 40% respectively. In the targeted delivery system of the present embodiment, the molar ratio of (D-Asp8)-SH to liposome is 10:100, the mass ratio of microRNA blocking a...

Embodiment 3

[0063] An embodiment of the small nucleic acid drug-based osteoclast targeted delivery system of the present invention, the small nucleic acid drug-based osteoclast targeted delivery system in this embodiment includes liposomes and eight gates with thiol-modified ends Blocker of aspartic acid polypeptide repeat ((D-Asp8)-SH) and microRNA. Wherein, liposome is made up of the lipid of following mass percent: 1,2-dioleyloxy-3-trimethylaminopropane (DOTAP) 5%, N-[1-(2,3-dioleyloxy) Propyl]-N,N,N,-trimethylammonium chloride (DOTMA) 10%, phosphatidylcholine (PC) 50%, DC-cholesterol (DC-Chol) 30% and distearoylphosphatidylethanolamine- Polyethylene glycol 2000-maleimide (DSPE-PEG-MAL) 5%; the microRNA blocking agent is composed of antagomir-214 and antagomir-2861 with mass percentages of 50% and 50%, respectively. In the targeted delivery system of the present embodiment, the molar ratio of (D-Asp8)-SH to liposome is 5:100, the mass ratio of microRNA blocking agent to liposome is 20...

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Abstract

The invention relates to the field of biopharmacy, and in particular relates to an osteoclast targeting delivery system based on a small nucleic acid medicine and a preparation method of the osteoclast targeting delivery system, used for regulating the functions of the osteoclasts. The osteoclast targeting delivery system comprises lipidosome, osteoclast targeting molecules and the small nucleic acid medicine used for regulating the functions of the osteoclasts. The delivery system carries out targeting aiming at the osteoclasts, thus having relatively strong specificity; the delivery system can prevent the small nucleic acid medicine from being degraded by the substance in the body, and also can specifically deliver the small nucleic acid medicine into target cells, and thus the functions of the osteoclasts can be regulated by the small nucleic acid medicine.

Description

technical field [0001] The invention relates to an osteoclast targeted delivery system and a preparation method thereof, in particular to a small nucleic acid drug-based osteoclast targeted delivery system and a preparation method thereof. Background technique [0002] Bone tissue resorption is the basic process of osteogenesis, and osteoclasts are responsible for this function. In osteoclasts, the abnormal expression of small nucleic acids can cause abnormal function of osteoclasts and various bone and joint diseases, such as osteoporosis, osteonecrosis and osteosclerosis. [0003] Small nucleic acids can regulate gene expression, thereby affecting cellular function. In recent years, a series of small nucleic acids that can regulate osteoclast function have been discovered, including the miR-29 family, miR-148a and miR-503 that affect osteoclast formation, migration and maturation. The discovery of small nucleic acid drugs that regulate osteoclasts has made it possible fo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K48/00A61K9/127A61K47/42A61P19/08
Inventor 张保亭刘振丽党蕾刘进郭保生
Owner BEIJING HELI CONSULTING CO LTD
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