Preparation method of amphiphilic biodegradable drug-loading micelle

A drug-loaded micelle, amphiphilic technology, applied in the fields of botanical equipment and methods, chemicals for biological control, biocides, etc. The problem of low utilization rate of ingredients, etc., achieves the effect of obvious dispersibility and effectiveness, improved water dispersibility, and improved efficacy

Active Publication Date: 2018-12-18
TSINGHUA UNIV
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Problems solved by technology

CN107714646A discloses an amphiphilic polymer micelle capable of penetrating tumor extracellular matrix and its preparation method. The amphiphilic polymer adopts block copolymerization obtained by copolymerization of polylactic acid or polycaprolactone and polyethylene glycol The drug-loaded micelles can enter the tumor site, but the drug-loading rate is relatively low, and the improvement of drug efficacy is relatively limited.
CN102408497A discloses a nanometer drug-loaded micelle solution with grafted carboxymethyl chitosan as a carrier. The micelle solution prepared by this method is uniform and stable, but the micelles cannot be given environmental responsiveness through chain structure regulation, and

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  • Preparation method of amphiphilic biodegradable drug-loading micelle
  • Preparation method of amphiphilic biodegradable drug-loading micelle
  • Preparation method of amphiphilic biodegradable drug-loading micelle

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preparation example Construction

[0030]A method for preparing amphiphilic biodegradable drug-loaded micelles proposed by the present invention comprises the following steps:

[0031] (1) Use the amphiphilic biodegradable block copolymer as the loading material, and dissolve the loading material and the drug to be coated in an organic solvent in proportion as an oil phase solution, wherein the ratio of the drug to be coated to the loading material is For: active pharmaceutical ingredient to be coated: loading material = 1: (0.25-10), the mass volume concentration of the loading material in the organic solvent is 1-50 mg / ml;

[0032] (2) Prepare amphiphilic biodegradable drug-loaded micelles by dialysis or film hydration, the specific steps of the two methods are as follows:

[0033] (2-1) Dialysis method: Measure deionized water equivalent to the oil phase solution described in step (1), and add deionized water dropwise to the oil phase solution under the process conditions of constantly stirring the oil phase...

Embodiment 1

[0045] Polybutylene methyl succinate-polyethylene glycol block copolymer (PBMS-PEG) (wherein the mass fraction of polyethylene glycol is 50% and the molecular weight of polyethylene glycol is 1000) synthesized in the laboratory at room temperature ) 20 milligrams and 2 milligrams of ibuprofen were dissolved in 4 milliliters of acetone as the oil phase; measure 4 milliliters of deionized water, and under constant stirring process conditions, added dropwise in the oil phase to form a stable, transparent and uniform oil-water Mixed solution; place the oil-water mixed solution in the corresponding dialysis bag for dialysis, replace fresh deionized water every 12 hours until the organic solvent is completely removed, and obtain a uniform and stable amphiphilic biodegradable pharmaceutical micelle solution after 3 days. Add water and dilute to 0.05 mg / ml to obtain the final amphiphilic biodegradable liquid pharmaceutical micelles, or freeze-dry the above-mentioned amphiphilic biodegr...

Embodiment 2

[0048] Polybutylene methylsuccinate-polyethylene glycol block copolymer (PBMS-PEG) (wherein the mass fraction of polyethylene glycol is 30% and the molecular weight of polyethylene glycol is 5000) synthesized in the laboratory at room temperature ) 20 mg and 2 mg of ibuprofen were dissolved in 4 milliliters of dimethyl sulfoxide (DMSO) as the oil phase; 4 milliliters of deionized water was measured, and added dropwise to the above oil phase under constant stirring process conditions, Form a stable, transparent and uniform oil-water mixture; place the oil-water mixture in the corresponding dialysis bag for dialysis, replace fresh deionized water every 4 hours until the organic solvent is completely removed, and obtain uniform and stable amphiphilic organisms after 3 days Degradable pharmaceutical micelles solution, diluted with water to 0.1 mg / ml to obtain the final amphiphilic biodegradable liquid pharmaceutical micelles, can also be freeze-dried above-mentioned amphiphilic bio...

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Abstract

The invention relates to a preparation method of an amphiphilic biodegradable drug-loading micelle, which belongs to the technical field of drug preparations. The preparation method comprises the following steps: adopting amphiphilic biodegradable segmented copolymer as a loading material, dissolving the loading material and to-be-coated drug according to a ratio in an organic solvent to beservedas an oil phase solution, wherein the ratio of the to-be-coated drug to the loading material is 1: (0.25 to 10), and the mass volume concentration of the loading material in the organic solvent is 1 to 50 mg/ml; and preparing the amphiphilic biodegradable drug-loading micelle by adopting a dialysis method or a film hydration method. The preparation obtained by adopting the method provided byof theinvention has the advantages of stability in storage, safety in transportation and application, good dispersity of compound dispersion solution and the like; and the obtained amphiphilic biodegradable pesticide micelle is high in leaf remaining amount, good in dispersity, and haswide in application prospect in the fields of pesticide spraying, seed mixing and the like.

Description

technical field [0001] The invention relates to a preparation method and application of a drug-loaded micelle with an amphiphilic biodegradable block copolymer as a loading material. By modifying part of the functional groups of the copolymer, it can respond to different environmental changes and achieve The purpose of controlling the release of medicine belongs to the technical field of pharmaceutical preparations. Background technique [0002] Most of the active ingredients of drugs are poorly water-soluble molecules, and it is usually necessary to improve the dispersibility of the drug to improve the effectiveness of the drug and reduce the side effects of the drug. Therefore, it is an effective method to improve the dispersibility of drugs to nanometerize the active ingredients of drugs. Traditional pharmacy solubilization methods include ultra-fine pulverization, adding solubilizers, changing the chemical structure of insoluble drugs, etc., but some of the above method...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K9/107A01N25/10A01N43/90A01N57/14A01N57/12A01N53/08A01N43/56A01P7/00
CPCA01N25/10A01N43/56A01N43/90A01N53/00A01N57/12A01N57/14A61K9/1075A61K47/34
Inventor 郭宝华韩佳睿徐军陈通李婷谢智宁郑天泽
Owner TSINGHUA UNIV
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