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A kind of polycaprolactone-polyethylene glycol nanomicelle loaded with hydrophobic antibiotic and its preparation and application

A technology of nanomicelle and polycaprolactone, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, and antibacterial drugs, can solve the problem that the delivery system is unstable and cannot play a targeting role. and other problems to achieve the effect of improving in vivo stability, increasing drug intake, and ensuring stability

Active Publication Date: 2021-10-22
SHANGHAI JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to overcome the existing problems in the use of existing antibiotic preparations, such as the unstable in vivo delivery system of existing hydrophobic antibiotics, which cannot play a targeting role, the object of the present invention is to provide a hydrophobic antibiotic-loaded polycaprolactone- Polyethylene glycol nano-micelle and its preparation and application

Method used

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  • A kind of polycaprolactone-polyethylene glycol nanomicelle loaded with hydrophobic antibiotic and its preparation and application
  • A kind of polycaprolactone-polyethylene glycol nanomicelle loaded with hydrophobic antibiotic and its preparation and application
  • A kind of polycaprolactone-polyethylene glycol nanomicelle loaded with hydrophobic antibiotic and its preparation and application

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Embodiment 1

[0048] Embodiment 1 carries the preparation method of erythromycin micelles

[0049] The drug loading is the percentage of the mass of erythromycin to the mass of the polymer carrier material.

[0050] The polymer carrier material PCL used in this embodiment 2000 - MPEG 2000 and PCL 5000 -PEG 2000 The molecular weights are: PEG and MPEG are both 2000Da, and PCL is 2000Da and 5000Da.

[0051] For a schematic diagram of the synthesis construction, see figure 1 .

[0052] The preparation method of blank micelles, comprises the steps:

[0053] the PCL 2000 - MPEG 2000 and PCL 5000 -PEG 2000 Mix according to the mass ratio of 0:1, 0.1:1, 0.3:1, 0.5:1, 0.8:1, 1:1, 1:0, co-dissolve in 10mL tetrahydrofuran and shake until completely dissolved and mix well; then follow the method of tetrahydrofuran and Deionized water volume ratio (3-9): 1 Add deionized water drop by drop. Remove tetrahydrofuran by rotary evaporation in a round-bottomed flask at 30-50°C under vacuum to obta...

Embodiment 2

[0059] The preparation method of embodiment 2 loaded erythromycin micelles

[0060] The preparation method of loading erythromycin micelles, comprises the steps: the PCL 2000 - MPEG 2000 and PCL 5000 -PEG 2000 Mix according to the mass ratio of 0.5:1, then add 1%, 5%, 10%, 15%, 20%, 25% of the total mass of the polymer carrier material erythromycin, dissolve in 2mL chloroform and shake until completely dissolved and Mix well; then add deionized water dropwise according to the volume ratio of deionized water to chloroform 1: (5-10). Remove chloroform by rotary evaporation in a round bottom flask at 30-50°C under vacuum to obtain a pan-opalescent micellar solution, and then sonicate in a water bath at 65°C for 10 minutes to further form a uniform micellar system. After filtering through a 0.22 μm microporous membrane to remove unencapsulated drug (erythromycin), it can be stored at 4°C for subsequent experiments.

[0061] The particle size and polydispersity coefficient of ...

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Abstract

The invention discloses a polycaprolactone-polyethylene glycol nano-micelle loaded with hydrophobic antibiotics and its preparation and application. The micelle includes a hydrophobic antibiotic and a micelle carrier, and the nano-micelle has a core-shell Structure; the hydrophobic block polycaprolactone in the micelle carrier and the hydrophobic antibiotic jointly form the core part, and the hydrophilic block polyethylene glycol forms the shell part. The present invention uses the easy crystallization property of polycaprolactone to tightly wrap hydrophobic antibiotics to ensure the stability of the drug before reaching the target cells; the hydrophilic PEG shell and the amphiphilic polymer block copolymer The particle size of the formed micelles is about 200nm, which helps the micelles to avoid being recognized by the systemic reticuloendothelial system, and has a long-term circulation function. This antibiotic-loaded nano-micelle structure can significantly improve the in vivo stability of antibiotics, has certain targeting properties, and avoids side effects.

Description

technical field [0001] The invention belongs to the technical field of drug delivery, and relates to a hydrophobic antibiotic-loaded nano-micelle, in particular to a hydrophobic antibiotic-loaded polycaprolactone-polyethylene glycol nano-micelle and its preparation and application. Background technique [0002] Antibiotics such as β-lactams, aminoglycosides, macrolides, lincomycins, polypeptides, quinolones, and sulfonamides commonly used in clinic can inhibit or kill pathogenic microorganisms, and are important for the prevention and treatment of infectious diseases. important drugs. At present, antibiotics as antibacterial drugs account for a considerable proportion of clinical medication, but at the same time it is found that antibiotics will encounter problems such as poor water solubility and stability, low concentration at the lesion site, and strong toxic and side effects in the treatment of bacterial infections. The effective use of drugs will cause damage to human ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/34A61K31/7048A61P31/04
CPCA61K9/1075A61K31/7048A61K47/34A61P31/04
Inventor 杜子秀彭佳惠徐宇虹殷瑜
Owner SHANGHAI JIAOTONG UNIV
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