Drug-loaded polymer micelle, preparation thereof and preparation method thereof

A drug-loaded polymer, amphiphilic polymer technology, used in tumor applications, drug-loaded polymer micelles and their preparations, to achieve enhanced anti-tumor effects, high blood exposure, and improved pharmacokinetic characteristics. Effect

Active Publication Date: 2021-09-07
ASCENTAGE PHARMA SUZHOU CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Therefore, there is a need for a drug-loaded drug that can deliver high loads of Bcl-2 / Bcl-xL inhibitors to patients with desirable stability, encapsulation efficiency, particle size, particle size PDI and improved pharmacokinetic characteristics. There is still an unmet need for polymeric micelles and their formulations

Method used

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  • Drug-loaded polymer micelle, preparation thereof and preparation method thereof
  • Drug-loaded polymer micelle, preparation thereof and preparation method thereof
  • Drug-loaded polymer micelle, preparation thereof and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0137] Example 1: Preparation of drug-loaded polymer PEOz-PCL micelles of the present invention

[0138] Preparation process: First, 24 mg of compound A and 72 mg of amphiphilic block copolymer PEOz-PCL (molecular weight 2000-2000 Daltons) were completely dissolved in 42 ml of methanol: dichloromethane: water (65:35:8) mixed solvent , Measure 3ml of purified water and add it to the stirring solution. After stirring for 30min, the organic solvent is removed by rotary evaporation to obtain the initial solution of micelles. Dilute the initial solution of micelles with purified water to 10ml, and then pass through a 0.22μm PES filter membrane to remove large particles. Resuspend the drug-encapsulated micellar solution, add trehalose and freeze-dry to obtain the micellar powder for long-term storage.

Embodiment 2

[0139] Example 2: Preparation of drug-loaded polymer PEOz-PCL micelles that inhibit cell efflux in the present invention

[0140] Preparation process: first, 20mg of compound A, 62.49mg of amphiphilic block copolymer PEOz-PCL (molecular weight 2000-2000 Daltons), 4.73mg of TPGS were completely dissolved in 42ml of methanol: dichloromethane: water (65:35: 8) In the mixed solvent, measure 3ml of purified water and add it to the above solution which is being stirred, stir for 30 minutes and then remove the organic solvent by rotary evaporation to obtain the initial micellar solution. Dilute the initial solution of micelles with purified water to 10ml, and then pass through a 0.22μm PES filter membrane to remove large particles. Resuspend the drug-encapsulated micellar solution, add trehalose and freeze-dry to obtain the micellar powder for long-term storage.

Embodiment 3

[0141] Example 3: Preparation of tumor-targeting drug-loaded polymer PEOz-PCL micelles of the present invention

[0142] Preparation process: first, 10 mg of compound A, 31.25 mg of amphiphilic block copolymer PEOz-PCL (molecular weight 2000-2000 Daltons), 5.88 mg of OCT-PEG-DSPE were completely dissolved in 42 ml of methanol: dichloromethane: water ( 65:35:8) in the mixed solvent, measure 3ml of purified water and add it to the above solution which is being stirred, stir for 30min and then remove the organic solvent by rotary evaporation to obtain the initial micellar solution. Dilute the initial solution of micelles with purified water to 10ml, and then pass through a 0.22μm PES filter membrane to remove large particles. Resuspend the drug-encapsulated micellar solution, add trehalose and freeze-dry to obtain the micellar powder for long-term storage.

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Abstract

The invention discloses a drug-loaded polymer micelle, a preparation thereof and a preparation method thereof. The drug-loaded polymer micelle comprises or consists of a medicinal active ingredient and an amphiphilic polymer, wherein the mass ratio of the medicinal active ingredient to the amphiphilic polymer is about 1: 1 to about 1: 10, and the definition is described in the specification. The drug-loaded polymer micelle and the preparation thereof can be used in the field of medicines and have beneficial effects.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to drug-loaded polymer micelles and preparations thereof. composition. The present invention also relates to the preparation method of the drug-loaded polymer micelle and the application of the drug-loaded polymer micelle and its preparation in treating tumors of subjects. Background technique [0002] Many drugs are hydrophobic and have very little solubility in water. For these poorly water-soluble drugs, in order to obtain ideal formulations to achieve desired clinical use and therapeutic effects, it is necessary to increase their water solubility. Various methods and techniques are known in the art that can be used to increase the water solubility of hydrophobic drugs, including cyclodextrin inclusion, solid dispersion, micronization, use of solubilizers, and the like. In recent years, there have been researches on the use of amphiphilic polymers as carriers of poor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/675A61K47/34A61K47/64A61K9/19A61P35/00A61P39/06A61P27/02A61P35/02
CPCA61K9/107A61K47/34A61K47/64A61K31/675A61P35/00A61P39/06A61P27/02A61P35/02A61K9/19
Inventor 林艳琼王晖李宗斌王光凤
Owner ASCENTAGE PHARMA SUZHOU CO LTD
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