Novel lung intelligent drug release system

A pulmonary and intelligent technology, applied in the field of drug release systems, can solve problems such as insufficient research, and achieve the effect of ensuring intelligent selectivity and improving bioavailability

Active Publication Date: 2020-08-25
杭州濡湜生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, a lot of research on targeted drug carriers has been carried out around the world, the main direction of which is concentrated on liposomes as carriers, and most of the research is mainly focused on liver-targeted drugs, while there is insufficient research on drug carriers in the lungs

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Phosphite Synthesis

[0035] Add anhydrous tetrahydrofuran (THF) under dry and nitrogen protection, cool to minus 78 degrees with dry ice, slowly add 78.5 grams of phosphorus trichloride (PCl 3 ) and 67.4 grams of 2,6-lutidine (2,6-lutidine), then 50 grams of 2-azide-ethanol was added dropwise, and the reaction mixture was stirred for 2 hours, during which the temperature rose from minus 78 degrees to minus 30 Spend. Recool the reaction mixture to minus 78 degrees, slowly add 67.4 grams of 2,6-lutidine (2,6-lutidine), then dropwise add 326 grams of diacylglycerol, and stir the reaction mixture for 5 hours, during which The temperature rose from minus 78 degrees to minus 20 degrees. Recool the reaction mixture to minus 78 degrees, slowly add 70 grams of 2,6-lutidine (2,6-lutidine), then slowly add water dropwise, and stir the reaction mixture for 1.5 hours, during which the temperature rises from minus 78 degrees to To minus 30 degrees, the reaction process...

Embodiment 2

[0036] Example 2: Phosphite Oxidation

[0037] The product of 100 grams of embodiment 1 is dissolved in 300 milliliters of toluene (toluene), is cooled to minus 10 degrees, then slowly adds dropwise 28 grams of sulfuryl chloride (SO 2 Cl 2 ), temperature remains no more than 0 degree, stirs 1 hour, removes excess sulfonyl chloride and solvent under reduced pressure distillation at low temperature, then adds 300 milliliters of tetrahydrofuran (THF) and dissolves and cools to zero degree, slowly adds 75 milliliters of water, stirs 3 Hours, the reaction process was monitored by TLC. After the reaction, the excess solvent was distilled off under reduced pressure, and the remaining solvent was dissolved in 600 ml of ethyl acetate, washed with saturated sodium chloride solution, dried over anhydrous sodium sulfate and concentrated to obtain 97 g of product.

Embodiment 3

[0038] Example 3: Reduction of azide group to amine

[0039] Dissolve 90 grams of the product of Example 2 in 300 milliliters of tetrahydrofuran (THF), add 98 grams of triphenylphosphine, raise the temperature to 50 degrees and keep for 3 hours, add dilute hydrochloric acid when the temperature drops to room temperature and stir for 2 hours, the reaction process uses TLC for monitoring. After the reaction, 600 ml of ethyl acetate was added, washed with saturated sodium bicarbonate solution and saturated sodium chloride solution, dried over anhydrous sodium sulfate and concentrated, then purified by column chromatography to obtain 79 g of product.

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PUM

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Abstract

The invention discloses a novel lung intelligent drug release system which comprises a targeted structure and a polypeptide adaptor, wherein the targeted structure is multivalent long-chain fatty acylphospholipid capable of being subjected to specific identification by a lung epithelial cell surface receptor SP-A; the polypeptide adaptor is used for connecting a drug with the targeted structure and is a polypeptide chain which can be specially hydrolyzed by specific protease; and the specific protease is expressed a lot only when lung cells have pathological features. According to the invention, the long-chain fatty acyl phospholipid is used as a specifically identified group so as to mediate cells to generate endocytosis, macromolecules in nucleic acid drugs or polypeptide drugs, which are difficult to pass through cell membranes, can be transferred into cells, and polypeptide which can be hydrolyzed by the specific protease expressed a lot at lung lesion sites is combined and used as the adaptor, so that the novel drug release system can enter lung cells in a targeted mode and intelligently identify the lung lesion sites to release the drug.

Description

technical field [0001] The invention relates to the technical field of drug delivery systems, in particular to a novel pulmonary intelligent drug delivery system. Background technique [0002] The lung intelligent drug delivery system contains two concepts, one is the lung targeting of the drug delivery system. The distribution of other organs in the human body, thereby reducing the dose and frequency of administration of drugs, reducing the side effects of drugs, has positive and important significance for the bioeffective utilization of drugs, drug compliance, drug safety and disease treatment methods; the second is The selectivity of the drug release system, the carrier is degraded by specific hydrolytic enzymes to release the active drug only when the lung cells are abnormal and pathological, and the drug will not be released for normal lung cells, thus ensuring the normal cells Not affected by drugs. [0003] At present, a lot of research on targeted drug carriers has...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/64A61K47/54
CPCA61K9/007A61K47/64A61K47/544
Inventor 王喆明谭昊
Owner 杭州濡湜生物科技有限公司
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