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RI7217 and muscone co-modification DTX long-circulation lipidosome, preparation method and application

A long-circulation liposome, RI7217 technology, applied in the field of medicine, can solve the problems of failing to enhance drugs and improve chemotherapy drugs

Pending Publication Date: 2021-04-20
康爽明
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] For this reason, the present invention provides a long-circulating liposome co-modified with RI7217 and muscone DTX, its preparation method and application to overcome the failure to enhance the BBB permeability of the drug in the prior art and efficiently target the brain glia Active brain-targeted delivery system for tumor cells and the problem of increasing the dose of chemotherapy drugs into the brain

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  • RI7217 and muscone co-modification DTX long-circulation lipidosome, preparation method and application
  • RI7217 and muscone co-modification DTX long-circulation lipidosome, preparation method and application
  • RI7217 and muscone co-modification DTX long-circulation lipidosome, preparation method and application

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[0060] In order to make the objects and advantages of the present invention clearer, the present invention will be further described below in conjunction with the examples; it should be understood that the specific examples described here are only for explaining the present invention, and are not intended to limit the present invention.

[0061] BBB: blood-brain barrier; RI7217: transferrin receptor monoclonal antibody RI7217; TfR: transferrin receptor; M: muscone; DSPE-PEG 2000 -Muscone: distearoylphosphatidylethanolamine-polyethylene glycol-muscarone; PEG-LP: long-circulating liposomes; M-LP: muscone-modified liposomes; RI7217-LP: RI7217-modified liposomes; RI7217-LP-M: liposomes co-modified with muscone and RI7217; DTX: docetaxel; PEG-LP-DTX: long-circulating liposomes loaded with docetaxel; M-LP-DTX: muscone loaded with docetaxel Modified liposome; RI7217-LP-DTX: RI7217 modified liposome loaded with docetaxel; RI7217-LP-M-DTX: co-modified liposome loaded with docetaxel mus...

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Abstract

The invention relates to a preparation method of RI7217 and muscone co-modification DTX long-circulation lipidosome. The preparation method comprises the following steps of: S1: firstly, carrying out amination modification on a muscone ring, and enabling the amination muscone and distearoyl phosphatidyl acetamide-N-hydroxy succinimide-polyethylene glycol to react to synthesize and prepare distearoyl phosphatidyl ethanolamine-polyethylene glycol-muscone; and S2: taking distearoyl phosphatidyl ethanolamine-polyethylene glycol-maleimide maleophthalimide, distearoyl phosphatidyl ethanolamine-polyethylene glycol, distearoyl phosphatidyl ethanolamine-polyethylene glycol-muscone copolymers, egg yolk lecithin and cholesterol as materials, preparing the lipidosome by a film dispersion method, and then, through covalent linkage of a maleimide group on the surface of the lipidosome and sulfhydrylation RI7217, preparing RI7217-LP and RI7217-LP-M.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a DTX long-circulation liposome co-modified with RI7217 and muscone, a preparation method and an application. Background technique [0002] Glioma is one of the most common intracranial tumors. Postoperative chemotherapy can prolong the survival period of patients and improve the quality of life of patients, so it is an indispensable treatment. However, due to the existence of the blood-brain barrier (BBB), it is difficult for conventional chemotherapeutic drugs to reach an effective therapeutic concentration in the brain through the BBB. Drug delivery. The study of microparticle drug delivery system through receptor-mediated brain targeting has the most advantage. Invented an active brain-targeted delivery system that can enhance the BBB penetration rate of drugs and efficiently target glioma cells, increase the amount of chemotherapy drugs entering the brain, and have a positive effe...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K47/68A61K47/69A61K31/337A61P35/00C08G65/333
Inventor 康爽明
Owner 康爽明
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