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Preparation method of polyethylene glycol monomethyl ether-polyester diblock copolymer micelles and drug-loaded micelles

A technology of polyethylene glycol monomethyl ether and block copolymer, which is applied in the field of polymers, can solve problems such as being unsuitable for large-scale production, and achieve the effects of improving encapsulation efficiency and solubility, easy storage, and small particle size.

Active Publication Date: 2017-04-19
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Dialysis and electrostatic interaction methods, not suitable for large-scale production

Method used

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  • Preparation method of polyethylene glycol monomethyl ether-polyester diblock copolymer micelles and drug-loaded micelles
  • Preparation method of polyethylene glycol monomethyl ether-polyester diblock copolymer micelles and drug-loaded micelles
  • Preparation method of polyethylene glycol monomethyl ether-polyester diblock copolymer micelles and drug-loaded micelles

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[0036] The embodiment of the present invention discloses a preparation method of drug-loaded nano micelles, comprising the following steps:

[0037] (A) Add the mixture of small molecule drug and organic solvent dropwise to polyethylene glycol monomethyl ether-polyester diblock copolymer to obtain a mixed solution;

[0038] (B) adding ultrapure water dropwise to the mixed solution while stirring for the first time, and after continuing the second stirring, dialysis to remove the organic solvent and freeze-drying to obtain drug-loaded nanomicelles;

[0039] The polyethylene glycol monomethyl ether-polyester diblock copolymer is shown in formula (I),

[0040]

[0041] Among them, -R- is or

[0042] m is the degree of polymerization, 10≤m≤900, preferably 20≤m≤800, more preferably 30≤m≤300; n is the degree of polymerization, 10≤n≤420, preferably 20≤n≤300, more preferably 40≤n≤250.

[0043] The present invention adopts the nano-sedimentation method to prepare the drug-loa...

Embodiment 1～5

[0064] Preparation of polyethylene glycol monomethyl ether-poly(D-lactide) diblock copolymers initiated by polyethylene glycol monomethyl ether with different number-average molecular weights

[0065] Weigh 1.67g, 3.33g, 6.67g, 16.67g, and 33.33g of polyethylene glycol monomethyl ether (MPEG) with molecular weights of 500, 1000, 2000, 5000, and 10,000, respectively, and put them into reaction flasks, and remove water by azeotropy. Add 12g of dextrolactide (DLA) in an anhydrous and oxygen-free environment, ventilate, the volume of toluene (mL) is 10 times the weight of ester monomer (g) 120mL, stannous octoate and ester monomer The molar ratio is 1 / 1000, inject 1 mL of 0.1 mol / L stannous octoate solution in toluene with a syringe, and put it in an oil bath at 120°C for 24 hours. After the reaction is complete, wait for the solution to cool down and settle with 1200mL of diethyl ether while stirring. The ratio of diethyl ether to toluene is 10 / 1. Filter the product through a Buc...

Embodiment 6～9

[0070] Preparation of polyethylene glycol monomethyl ether-poly(D-lactide) diblock copolymers with different degrees of polymerization initiated by polyethylene glycol monomethyl ether

[0071] Weigh 4g, 6g, 8g, and 12g of polyethylene glycol monomethyl ether (MPEG) with a molecular weight of 5000 and put them into a reaction bottle, remove water by azeotropic addition, and add dextrolactide (DLA) in an anhydrous and oxygen-free environment. ) 12g, ventilation, the volume of toluene (mL) is 10 times the weight of ester monomer (g) 120mL, the molar ratio of stannous octoate and ester monomer is 1 / 1000, inject 0.1mol / L octanoic acid with a syringe Put 1mL of stannous toluene solution in an oil bath at 120°C for 24h. After the reaction is complete, wait for the solution to cool down and settle with 1200mL of diethyl ether while stirring. The ratio of diethyl ether to toluene is 10 / 1. Filter the product through a Buchner funnel. Dissolve the product in chloroform and settle it wit...

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Abstract

The invention provides a preparation method of drug-loaded nano-micelles: adding dropwise a mixture of a small molecule drug and an organic solvent into a polyethylene glycol monomethyl ether-polyester diblock copolymer to obtain a mixed solution; The mixed solution was stirred for the first time while adding ultrapure water dropwise, and after the second stirring was continued, the organic solvent was removed by dialysis and freeze-dried to obtain drug-loaded nano micelles. The present invention also provides a preparation method of polyethylene glycol monomethyl ether-polyester diblock copolymer micelles: dissolving polyethylene glycol monomethyl ether-polyester diblock copolymer in an organic solvent, While stirring for the first time, ultrapure water was added dropwise, and after stirring for the second time, the organic solvent was removed by dialysis and freeze-dried to obtain diblock copolymer micelles. The micelles prepared by this method are easy to operate, under mild conditions, and present a good monodisperse state, which can encapsulate small molecule drugs with poor water solubility, and improve the encapsulation efficiency and solubility of drugs, and the obtained drug-loaded nano-micelles have a stable structure , easy to store.

Description

technical field [0001] The invention relates to the field of macromolecules, in particular to a preparation method of polyethylene glycol monomethyl ether-polyester diblock copolymer micelles and drug-loaded micelles. Background technique [0002] Polymer carrier drug is an emerging drug delivery technology with the development of pharmaceutical research, biomaterial science and clinical medicine. Low-molecular-weight drugs have the advantages of high curative effect and convenient use, but they also have great side effects. Generally, low-molecular-weight drugs enter the human body through oral administration or injection, with fast metabolism, short half-life, and lack of selectivity. A polymer carrier drug refers to a polymer that has no pharmacological effect and does not react with the drug itself as a carrier of the drug. A class of drugs obtained on the chain. Among them, the high-molecular compound acts as a delivery system for low-molecular drugs. [0003] Using...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/34A61P35/00
Inventor 丁建勋刘东红庄秀丽陈学思
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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