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Kartogenin cartilage delivery material based on epsilon-polylysine as well as preparation method and kit thereof

A technology of polylysine and polylysine hydrochloride, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, bone diseases, etc., can solve the problem that it is difficult to really improve KGN intervention in arthritis biological Utilization etc.

Pending Publication Date: 2020-10-20
SHANGHAI SIXTH PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the existing technology prolongs the residence time of KGN in the joint cavity, KGN is still released into the joint cavity in the form of small molecule reagents and then penetrates into the cartilage tissue to play a role
Therefore, the existing technology has not fundamentally changed the problem of KGN's water solubility and rapid clearance in the joint cavity, and it is difficult to really improve the bioavailability of KGN for intervening arthritis

Method used

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  • Kartogenin cartilage delivery material based on epsilon-polylysine as well as preparation method and kit thereof
  • Kartogenin cartilage delivery material based on epsilon-polylysine as well as preparation method and kit thereof
  • Kartogenin cartilage delivery material based on epsilon-polylysine as well as preparation method and kit thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] This embodiment provides a Kartogenin cartilage delivery material based on ε-polylysine, which has a structure such as formula (I):

[0051]

[0052] Among them, R is:

[0053]

[0054] R 1 for:

[0055]

[0056] Among them, p and q are the collection of positive integers and 0, and 0≤p≤50, 0≤q≤20;

[0057] R 2 for: -H or

[0058]

[0059]

[0060] In a preferred embodiment, in formula (I), n is a positive integer, and 5≤n≤200.

[0061] In a preferred embodiment, in formula (I), a, b, and c are a set of positive integers and 0, and a≥0, and at least one of b and c is not 0.

[0062] In a preferred embodiment, in formula (I), a+b+c=n.

Embodiment 2

[0064] This embodiment provides the preparation method of the ε-polylysine-based Kartogenin cartilage delivery material having the structure of formula (I) when c=0 in the above-mentioned embodiment 1:

[0065] Accurately weigh 0.317g (1mmol) KGN and 0.26g (1.2mmol) 4-(4,6-dimethoxytriazin-2-yl)-4-methylmorpholine hydrochloride (DMTMM), fully dissolve In 15mL of DMF, stirred at 25°C for 2 hours; then, under the conditions of 5Pa and 60°C, the organic solvent DMF was evaporated, and the obtained solid powder was dissolved in 2mL of dichloromethane, and separated by column chromatography. The separation conditions were: : 200-300-mesh column chromatography silica gel, the eluent is a mixed solvent of dichloromethane / petroleum ether with a volume ratio of 1:2, and the yellow powder active intermediate with the structure of formula (II) is obtained.

[0066]

[0067] Accurately weigh 1g (the molar weight of the amino group is about 6.1mmol) of ε-polylysine hydrochloride (the de...

Embodiment 3

[0071] This example provides the preparation method of the epsilon-polylysine-based Kartogenin cartilage delivery material having the structure of formula (I) when a=0.6, b=0.2, and c=0.2 in the above-mentioned embodiment 1:

[0072] Kartogenin (0.32g, 0.1mmol), PEG polymer represented by formula (III) (p=5, q=1, 0.36g, 0.12mmol), dicyclohexylcarbodiimide (0.25g, 0.12mmol) and 4-dimethylaminopyridine (0.15g, 0.12mmol) were dissolved in anhydrous dichloromethane, stirred at 25°C for 25 hours; Compound 0.5g, yield 80%;

[0073]

[0074] Accurately weigh 1 g of polylysine hydrochloride (the molar weight of the amino group is about 6.1 mmol), dissolve it in 50 mL of water / N'N-dimethylformamide with a volume ratio of 1:1, and use 2M NaOH The pH of the solution was adjusted to between 8-9; then 0.56g (1.22mmol) of compound (II) and 1.4g (2.44mmol) of compound (IV) were added, and stirred at room temperature for 30 hours; then 50mL was added to the reaction solution to Ionized w...

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Abstract

The invention discloses a Kartogenin cartilage delivery material based on epsilon-polylysine and a preparation method thereof material. The cartilage delivery material is prepared by connecting Kartogenin molecules and epsilon-polylysine through covalent bonds. According to the cartilage delivery material, the residence time of KGN in an articular cavity can be prolonged, and the solubility of theKGN is improved; meanwhile, the material has cartilage permeability and cell membrane permeability, permeates into cartilage tissues and stem cells and cartilage cells in the cartilage tissues in anintegral material form, and is degraded under the action of intracellular enzymes to release the KGN, so that the bioavailability of the KGN is improved; and the tissue and cell compatibility is excellent, and the toxic and side effects cannot be caused. The invention also discloses a kit, freeze-dried powder of the Kartogenin cartilage delivery material is used as a component A, a biocompatible solvent is used as a component B, the use process is very simple, and the component A and the component B can be directly subjected to articular cavity injection administration after being mixed and dissolved.

Description

technical field [0001] The invention relates to the field of biological materials, in particular to a Kartogenin cartilage delivery material based on epsilon-polylysine, a preparation method and a kit thereof. Background technique [0002] Osteoarthritis is a disease characterized by degeneration of articular cartilage tissue as the main pathological feature, and joint pain and restricted movement function as the main clinical manifestations. With the aging population in our country, the number of patients with osteoarthritis has risen sharply. According to statistics, the incidence of arthritis in people over 40 years old in my country exceeds 40%. At present, the intervention of arthritis is mainly aimed at relieving pain and restoring function, and there is no clinical treatment drug to improve the pathological manifestations of arthritis. Kartogenin (KGN) is a small molecule TGF-β and Smad4 / 5 pathway inhibitor discovered in recent years, which can efficiently promote c...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K9/00A61K31/192C08G69/48A61P19/02A61P19/04
CPCA61K47/34A61K9/0019A61K31/192C08G69/48A61P19/02A61P19/04
Inventor 郑宪友杨云龙林俊卿
Owner SHANGHAI SIXTH PEOPLES HOSPITAL
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