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Construction of intravenous-injection self-assembled nano-particles of triglyceride prodrug

A technology of nanoparticles and prodrugs, which is applied in drug combinations, antineoplastic drugs, pharmaceutical formulations, etc., can solve problems such as side effects, achieve high-efficiency entrapment, good stability, and simple and easy preparation methods

Active Publication Date: 2021-03-16
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is a small amount of reducing substances in the blood circulation, so it is possible to release the parent drug early, causing side effects
However, there are no reports of ATGL-based stimuli-responsive drug delivery systems

Method used

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  • Construction of intravenous-injection self-assembled nano-particles of triglyceride prodrug
  • Construction of intravenous-injection self-assembled nano-particles of triglyceride prodrug
  • Construction of intravenous-injection self-assembled nano-particles of triglyceride prodrug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Synthesis of docetaxel-like triglyceride prodrug (DSSTG(0))

[0032] Weigh an appropriate amount of stearic acid, EDCI, and DMAP in a 100ml eggplant-shaped bottle, add 60ml of anhydrous dichloromethane to dissolve and activate it in an ice bath for half an hour, weigh an appropriate amount of 1,3-dihydroxyacetone and add it to the above reaction solution , under the protection of nitrogen, react at room temperature for 48h. After the reaction solution was spin-dried, the crude product was separated by silica gel column chromatography to obtain an intermediate product. Weigh an appropriate amount of the intermediate product and dissolve it in a mixed solvent of tetrahydrofuran and benzene, slowly add 2ml of deionized water to the syringe under stirring, slowly add an appropriate amount of sodium borohydride in an ice bath and continue the reaction for 30 minutes, and slowly add 0.5ml of acetic acid dropwise to terminate the reaction. Add 60ml of chloroform to t...

Embodiment 2

[0035] Example 2: Synthesis of docetaxel-like triglyceride prodrug (DSSTG(1))

[0036] Weigh an appropriate amount of oleic acid, EDCI, and DMAP into a 100ml eggplant-shaped bottle, add 60ml of anhydrous dichloromethane to dissolve and activate it in an ice bath for half an hour, weigh an appropriate amount of 1,3-dihydroxyacetone and add it to the above reaction solution , Under the protection of nitrogen, react at room temperature for 48h. After the reaction solution was spin-dried, the crude product was separated by silica gel column chromatography to obtain an intermediate product. Weigh an appropriate amount of the intermediate product and dissolve it in a mixed solvent of tetrahydrofuran and benzene, slowly add 2ml of deionized water to the syringe under stirring, slowly add an appropriate amount of sodium borohydride in an ice bath and continue the reaction for 30 minutes, and slowly add 0.5ml of acetic acid dropwise to terminate the reaction. Add 60 ml of chloroform t...

Embodiment 3

[0039] Example 3: Synthesis of docetaxel-like triglyceride prodrug (DSSTG(2))

[0040] Weigh an appropriate amount of linoleic acid, EDCI, and DMAP into a 100ml eggplant-shaped bottle, add 60ml of anhydrous dichloromethane to dissolve and activate it in an ice bath for half an hour, weigh an appropriate amount of 1,3-dihydroxyacetone and add it to the above reaction solution , under the protection of nitrogen, react at room temperature for 48h. After the reaction solution was spin-dried, the crude product was separated by silica gel column chromatography to obtain an intermediate product. Weigh an appropriate amount of the intermediate product and dissolve it in a mixed solvent of tetrahydrofuran and benzene, slowly add 2ml of deionized water to the syringe under stirring, slowly add an appropriate amount of sodium borohydride in an ice bath and continue the reaction for 30 minutes, and slowly add 0.5ml of acetic acid dropwise to terminate the reaction. Add 60 ml of chlorofor...

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Abstract

The invention belongs to the fields of novel adjuvants and novel dosage forms of pharmaceutical preparations and relates to lipase-reducing-environment-programmed-triggered synthesis of a triglycerideprodrug, construction of intravenous-injection self-assembled nano-particles of the prodrug and application of the prodrug in drug delivery. According to the disulfide-bond-bridged triglyceride prodrug, Docetaxel is selected as a model drug and is connected to a structural framework of triglyceride through dithiodiglycolic acid, and fatty acids of 1 and 3 positions are (a) stearic acid, (b) oleicacid and (c) linoleic acid. The disulfide-bond-bridged triglyceride prodrug is designed and synthesized, and the synthesis method is easy and feasible; meanwhile, uniform micromolecular prodrug self-assembly nano-particles are prepared, the preparation method is easy and feasible, the stability is good, and the efficient entrapment of the Docetaxel is achieved; and the micromolecular prodrug self-assembly nano-particles of the triglyceride prodrug can be applied to injection administration, problems of Docetaxel injections in the prior art are overcome, and thus, the treatment effect is improved.

Description

technical field [0001] The invention belongs to the field of new excipients and new dosage forms of pharmaceutical preparations, including the synthesis of triglyceride-like prodrugs triggered by lipase reduction environment programming, the construction of self-assembled nanoparticles for intravenous injection of prodrugs, and its application in drug delivery . Background technique [0002] Cancer is a serious threat to human life. The number of cancer patients in the world is increasing year by year, and the mortality rate remains high. Chemotherapy is still the main way of clinical treatment of cancer, especially for tumors that are not easy to be removed by surgery and easy to spread. However, most of the chemotherapeutic drugs belong to the BCS Ⅳ class of drugs, which have the characteristics of low solubility and poor permeability, and the chemotherapeutic drugs also have disadvantages such as poor stability in vivo, high toxicity, and narrow therapeutic window. At p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/54A61K31/337A61P35/00
CPCA61K9/5123A61K47/543A61K31/337A61P35/00
Inventor 孙进何仲贵田楚彤
Owner SHENYANG PHARMA UNIVERSITY
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