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Method for efficiently loading medicines in cell membrane microcapsules

A cell membrane, medium and high-efficiency technology, which is applied in the direction of pharmaceutical formulas, medical preparations of non-active ingredients, inorganic non-active ingredients, etc., can solve the problems of poor permeability of the capsule wall and only specific molecules can be loaded, and increase the permeability , Superior biocompatibility and transfer performance, and the effect of simple process

Inactive Publication Date: 2014-07-16
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, cell membrane microcapsules also have the disadvantages of poor permeability of the capsule wall and can only load specific molecules.

Method used

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  • Method for efficiently loading medicines in cell membrane microcapsules
  • Method for efficiently loading medicines in cell membrane microcapsules
  • Method for efficiently loading medicines in cell membrane microcapsules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] 1) Add 20 μL of cytochalasin b solution (concentration: 1 mg / mL) to the culture dish of human vascular endothelial cells, incubate at 37°C for 30 minutes, wash with phosphate buffer three times, digest with trypsin, and collect cells by centrifugation; The obtained cells were vortexed for 1 min; the supernatant collected by centrifugation was the cell membrane microcapsule suspension.

[0022] Disperse 200 μg of the cell membrane microcapsules obtained above in 1 mL of phosphate buffer; add 10 μL of 1 mg / mL cell membrane red dye DiI to it, mix well, and incubate for 15 min; centrifuge and wash the obtained cell membrane microcapsules several times to remove unlabeled The dye on the membrane; see the fluorescent photo of the cell membrane microvesicles dispersed in phosphate buffered saline figure 1 .

[0023] 2) Add 200 μg of the cell membrane microcapsules obtained in step 1) into the mixed solution of digitonin and doxorubicin hydrochloride, so that the concentration...

Embodiment 2

[0025] Same as Example 1, the difference lies in step 2), take 200 μg of the cell membrane microcapsules obtained in step 1) and add them to the mixed solution of digitonin and gadopentetate dimeglumine, so that the concentrations of digitonin and gadopentetate dimeglumine 10μg / mL and 200μg / mL respectively, incubate at 37°C for 3~24h; add calcium chloride solution to make the calcium ion concentration 5mM, incubate at 37°C for 2h; centrifuge and wash with phosphate buffer three times to obtain gadopentetate-loaded Cell membrane microcapsules of meglumine. According to inductively coupled plasma mass spectrometry, the drug concentration in the microcapsules is 0.8, 2, 16.2 μg / mL, see image 3 .

Embodiment 3

[0027] Same as Example 1, the difference lies in step 2), take 200 μg of the cell membrane microcapsules obtained in step 1) and add them to the mixed solution of digitonin and fluorescein-labeled dextran (molecular weight 4kD), so that digitonin and glucosinolate The concentrations of glycans were 10 μg / mL and 200 μg / mL, and incubated at 37°C for 3-24h; calcium chloride solution was added to make the calcium ion concentration 5mM, and incubated at 37°C for 2h; centrifuged and washed with phosphate buffer three times to obtain Cell membrane microcapsules loaded with dextran. According to the peak intensity of excitation at 488nm and emission at 525nm in the fluorescence spectrogram, the concentrations of fluorescein-modified dextran in the microcapsules are respectively 0.8, 0.9, and 1.1 μg / mL, see Figure 4 .

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Abstract

The invention discloses a method for efficiently loading medicines in cell membrane microcapsules. The method comprises the following steps: preparing the cell membrane microcapsules by using human vascular endothelial cells as raw materials; soaking the obtained cell membrane microcapsules in a mixed solution of digitonin and medicines, wherein the digitonin is capable of increasing the cell membrane permeability, and the medicines penetrate into the cell membrane microcapsules; using calcium ions for sealing the cell membranes, thus obtaining the medicine-loading cell membrane microcapsules. The preparation method disclosed by the invention is simple, convenient, controllable, fast in speed, high in production efficiency and capable of conveniently loading the multiple medicines in the cell membrane microcapsules and adjusting the medicine-loading capacity of the cell membrane microcapsules and has good application prospect.

Description

technical field [0001] The invention relates to a method for efficiently loading drugs in cell membrane microcapsules. In particular, the use of digitonin to increase cell membrane permeability and the use of calcium ions to seal the cell membrane after drug loading. Background technique [0002] Efficient loading and controlled release of drugs in carriers is an important prerequisite for effective drug utilization and reduced toxicity. The loading of drugs in the carrier can protect the drug and improve its stability; at the same time, it can regulate the release rate and location of the drug, reducing its toxicity to healthy cells and tissues. [0003] Common drug carriers mainly use artificially synthesized polymers or naturally derived proteins and polysaccharides as raw materials, and their structures are relatively simple. However, they often have poor biocompatibility, are easily recognized and cleared by the human immune system, have short circulation time in the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/46A61K47/26A61K47/02
Inventor 毛峥伟张元洪
Owner ZHEJIANG UNIV
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