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Mannose receptor targeted composition, medicine and preparation method and application of mannose receptor targeted composition

A composition, mannose technology, applied in the field of nano-preparation composition, can solve the problems of normal tissue damage during heating time, lower utilization rate, no active targeting, etc., to achieve precise targeted therapy and good tumor target tropism effect

Active Publication Date: 2019-12-03
CHENGDU RIBOCURE PHARMATECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thermosensitive liposomes can directly kill tumor cells, but heating for too long can also cause damage to normal tissues
Molecularly targeted liposomes also have problems such as directional delivery of drugs and poor absorption of target organs in vivo.
[0005] In summary, the primary problem to be solved in the research and development of targeted drugs is to maintain the stability of nanocarriers during transportation without being destroyed. Ordinary nanoparticles or liposomes do not have active targeting (some may have passive targeting). sex), easy to be cleared by the endothelial system, reducing the utilization rate, and may cause unnecessary toxic and side effects

Method used

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  • Mannose receptor targeted composition, medicine and preparation method and application of mannose receptor targeted composition
  • Mannose receptor targeted composition, medicine and preparation method and application of mannose receptor targeted composition
  • Mannose receptor targeted composition, medicine and preparation method and application of mannose receptor targeted composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0099] Example 1 is used to prepare the composition of the nano-preparation with targeting function

[0100]

[0101]

[0102] The material of lipid is cholesterol, egg yolk lecithin, soybean lecithin, cephalin, sphingomyelin, PC (phosphatidylcholine), EPG (egg phosphatidylglycerol), SPG (soybean phosphatidylglycerol), Distearoylphosphatidylethanolamine (DSPE), dipalmitoylphosphatidylethanolamine (DPPE), dipalmitoylphosphatidylcholine (DPPC), dioleoylphosphatidylcholine (DOPC), distearoylphosphatidylcholine Alkaline (DSPC), Dimyristoylphosphatidylcholine (DMPC), Dilinoleoylphosphatidylcholine (DLPC), Dioleoylphosphatidylglycerol (DOPG), Dipalmitoylphosphatidylglycerol (DPPG), Dimely Myristoylphosphatidylcholine (DMPC), Dilauroylphosphatidylglycerol (DLPG), Cetyltrimethylammonium Bromide (CTAB), Dimethyl Dioctadecylammonium Bromide (DDAB), One or more of 1,2-dioleoyl-3-trimethylammoniumpropane (chloride salt) (DOTAP).

[0103] In this embodiment, the amino acid of the s...

Embodiment 2

[0104] Example 2 Preparation of Targeting Vector

[0105] The basic nano-preparation material in Example 1 is prepared into a nano-drug delivery carrier, and then the targeting material in Example 1 is attached to the surface of the prepared nano-drug delivery carrier to obtain a targeting carrier.

Embodiment 3

[0106] Embodiment 3 prepares targeted drug

[0107] The drug is wrapped in the targeting carrier prepared in Example 2.

[0108] In this embodiment, the drugs are small molecule drugs and / or protein and polypeptide drugs and / or gene drugs.

[0109] The small molecular drugs are antineoplastic drugs taxanes (paclitaxel, docetaxel, cephalomannine, 7-epitaxel), camptothecins (camptothecin, SN38, irinotecan, 9- Aminocamptothecin, 9-nitrocamptothecin, etc.), vinblastine (vinblastine, vincristine, vindesine, vinorelbine, vinflunine, etc.), adriamycin, epirubicin, dauna Erythromycin, epirubicin, amphotericin, methotrexate, cytarabine, 5-fluorouracil, mitoxantrone or its derivatives, gefitinib, noscapine, cisplatin, card Platinum, oxaliplatin, carmustine, quercetin, etc.

[0110] The main ingredient protein polypeptide drugs are interleukins (such as IL-1, IL-1a, IL-2, IL-3, IL-4, IL-5, IL-6, etc.), various growth factors ( Such as fibroblast growth factor, liver growth factor, va...

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Abstract

The invention belongs to the field of medicinal preparations, and particularly relates to a composition of a nanometer preparation having a targeting function, a targeting carrier and a preparation method thereof, a targeting medicine and a method for improving targeting properties of the targeting carrier. The composition of the nanometer preparation having a targeting function consists of a targeting material, a basic nanometer preparation material, and an interval material enabling the targeting material and the basic nanometer preparation material to produce distances. The targeting nanometer preparation has better mannose receptor targeting properties and can be efficiently combined with a mannose receptor on a target cell; and besides, the preparation method has generality, various targeting nanometer preparations can be synthesized, and purification and representation are facilitated.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a nano-preparation composition with a targeting function, a targeting carrier and a preparation method thereof, a targeting drug and a method for improving the targeting of the targeting carrier. Background technique [0002] In recent years, drug receptor-mediated targeted drug delivery systems have been extensively studied. Targeted drug delivery systems can improve their specific targeting and overcome the problems of wide distribution of drugs in vivo and serious side effects. Among them, lectin receptors are a kind of glycoproteins, glycolipids or carbohydrate complexes distributed on the surface of cell membranes, which can specifically recognize and bind to some sugar groups. Mannose receptor is the most important high-efficiency endocytic lectin receptor. Its functions include clearing endogenous molecules, promoting antigen presentation, and regulat...

Claims

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Application Information

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IPC IPC(8): A61K47/26A61K47/10A61K47/54A61K47/60A61K39/00A61K48/00A61K31/704A61K31/352A61K31/337A61P35/00A61P9/10A61P29/00
CPCA61K47/26A61K47/10A61K47/549A61K47/60A61K39/00A61K48/005A61K31/704A61K31/352A61K31/337A61P35/00A61P9/10A61P29/00A61K9/127A61K47/6911A61K47/6917A61K47/6907A61K47/6929B82Y5/00A61K31/4745A61K31/475A61K31/7048A61K31/519A61K31/513A61K31/5377A61K31/17C12N15/88A61K48/0041A61K9/1271A61K47/34B82Y40/00
Inventor 宋相容魏于全
Owner CHENGDU RIBOCURE PHARMATECH CO LTD
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