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Polyethylene glycol derivative as well as preparation method and application thereof

A polyethylene glycol, polyethylene glycol group technology, applied in pharmaceutical formulations, cosmetic preparations, cosmetic preparations, etc., can solve the problem of reducing tissue penetration, large size, and affecting the kinetic accuracy of hydrophobic compounds. adjustment, etc.

Active Publication Date: 2020-07-17
天津力博生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, a large number of lipophilic and hydrophilic groups make the size of the block copolymer polymer micelles larger, and the hydration radius can reach more than 100 nm, which reduces the tissue penetration
Moreover, it is difficult to precisely control the distribution and number of hydrophobic chains in the copolymer, which affects the precise adjustment of the release kinetics of hydrophobic compounds.

Method used

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  • Polyethylene glycol derivative as well as preparation method and application thereof
  • Polyethylene glycol derivative as well as preparation method and application thereof
  • Polyethylene glycol derivative as well as preparation method and application thereof

Examples

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preparation example Construction

[0096] The preparation method of the present invention will be further described in detail in conjunction with specific examples below. It should be understood that the following examples are only for illustrating and explaining the present invention, and should not be construed as limiting the protection scope of the present invention. All technologies realized based on the above contents of the present invention are covered within the scope of protection intended by the present invention.

[0097] The molecular weight of diisopropylethylamine used in the following examples is 129 Da, and the manufacturer is Beijing Chemical Plant. used in the following examples N,N -Dimethylformamide is anhydrous DMF, the purity is analytically pure, and the manufacturer is Beijing Chemical Plant.

[0098] The experimental methods used in the following examples are conventional methods unless otherwise specified; the reagents and materials used in the following examples can be obtained fr...

Embodiment 1

[0102] Example 1 Synthesis of three aliphatic chain-polyethylene glycol derivatives (1DSPE, 1 n-octadecanethiol)

[0103] Weigh out 50 mg DSPE in a 10 mL round bottom glass flask and dissolve it in 100 µL N,N - In dimethylformamide, add 12 µL of diisopropylethylamine to obtain a solution (a).

[0104]Use a 2 ml weighing bottle to weigh 334 mg of end-group-substituted polyethylene glycol OPSS-PEG5000-SCM (polyethylene glycol with an average molecular weight of 5000 Da and end groups of dithiopyridyl and succinimide carboxymethyl ester respectively). Alcohol, purchased from Beijing Jiankai Technology Co., Ltd., product number A5109), was dissolved in 400 µL DMF to obtain solution (2).

[0105] The solution (2) was added into the round bottom flask with the solution (1) for mixing, stirred by magnetic force, and reacted at room temperature for 4 hours under the protection of nitrogen. Afterwards, nitrogen protection was removed, and 100 µL of 0.5 M hydrochloric acid solution w...

Embodiment 2

[0107] Example 2 Synthesis of three aliphatic chain-polyethylene glycol derivatives (1DSPE, 1 n-octyl thiol)

[0108] Weigh 50 mg of DSPE in a 10 mL round bottom glass flask, dissolve it in 100 µL of DMF, and add 12 µL of diisopropylethylamine to obtain solution (a).

[0109] Use a 2 ml weighing bottle to weigh 334 mg of terminal-substituted polyethylene glycol MAL-PEG5000-SCM (polyethylene glycol with an average molecular weight of 5000 Da and terminal groups of maleimide and succinimide carboxymethyl ester respectively). Diol, purchased from Beijing Jiankai Technology Co., Ltd., product number A5003), was dissolved in 400 µL DMF to obtain solution (2).

[0110] Add 15 µL of 1-octanethiol (molecular weight 146, purchased from Beijing Bailingwei Technology) to solution (2), and react for 1 hour under nitrogen protection. The obtained reaction solution was added into the round bottom flask with solution (1) for mixing, stirred by magnetic force, and reacted for 4 hours at room...

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Abstract

The invention provides a polyethylene glycol derivative as well as a preparation method and application thereof, wherein the polyethylene glycol derivative comprises a group containing an aliphatic chain and polyethylene glycol, the group containing the aliphatic chain is connected with the polyethylene glycol through a connecting group, and at least one group in the group containing the aliphaticchain is a phospholipid group. A hydrophobic part (namely lipophilic group) can be used for adjusting the volume and association strength of the hydrophobic part by changing the chain length, saturation and number of aliphatic chains; the volume of the hydrophilic part can be adjusted by selecting the chain length and the branch number of polyethylene glycol macromolecules, and stable micelles with different micelle sizes can be obtained through the synergistic cooperation of the hydrophobic part and the hydrophilic part.

Description

technical field [0001] The invention relates to a polyethylene glycol derivative, a preparation method thereof, and an application in hydrophobic compound coating and delivery, and belongs to the technical field of lipid molecules. Background technique [0002] After the surfactant containing hydrophilic groups and lipophilic groups reaches and exceeds a specific concentration in the solution, the molecules automatically associate into colloid-sized aggregate particles called micelles, and the specific concentration is called the critical micelle concentration (CMC) . The formation of micelles is an entropy-driven process. When a single surfactant molecule is completely surrounded by water molecules in water, the degree of freedom of water molecules at the contact interface between lipophilic groups and water molecules decreases sharply, which causes the entropy of the mixed system to decrease and become a thermodynamically unstable state. In order to maintain the total ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/335C08G65/334C08G65/333A61K8/06A61K8/86A61K9/107A61K47/10A61Q19/00
CPCA61K8/06A61K8/86A61K9/1075A61K47/10A61Q19/00C08G65/33306C08G65/334C08G65/3353C08G2650/50
Inventor 王晓
Owner 天津力博生物科技有限公司
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