A kind of preparation method of amphiphilic biodegradable drug-loaded micelles

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...

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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 different Controlled Release in Circumstances

CN107236100A discloses a preparation method of a pH-stimulus-responsive linear diblock polymeric prodrug. The polymer prodrug prepared by the method has the advantages of high drug loading and pH-stimulus responsiveness, but the synthesis process is complicated, which is not conducive to Large-scale promotion in the field of drug loading, especially pesticides

The active ingredients of broad-spectrum pesticides such as abamectin and lambda-cyhalothrin are also low in the utilization rate of active ingredients due to the dispersion of insoluble drugs. At the same time, they are easy to cause environmental pollution and endanger the health of pesticide applicators.

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