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Folate-targeted hydrophobic medicine-loaded polymeric vesicle and preparation method and use thereof

A hydrophobic drug and folic acid targeting technology, applied in drug combination, pharmaceutical formula, drug delivery, etc., can solve the problems of high toxicity and side effects, unsatisfactory treatment effect, etc., and achieve strong permeability, high strength, and good stability Effect

Inactive Publication Date: 2011-01-26
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Malignant tumors are serious diseases that threaten human health. After the general administration form of chemotherapy drugs enters the body, due to the systemic distribution of the drugs, the toxic and side effects are large, and the therapeutic effect is not ideal. Therefore, tumor treatment especially requires a drug delivery system for targeted delivery.

Method used

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  • Folate-targeted hydrophobic medicine-loaded polymeric vesicle and preparation method and use thereof
  • Folate-targeted hydrophobic medicine-loaded polymeric vesicle and preparation method and use thereof
  • Folate-targeted hydrophobic medicine-loaded polymeric vesicle and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] A folic acid-targeted hydrophobic drug-loaded polymer vesicle is prepared by the following method:

[0043] (1) Dissolve the PCL-b-PEG-b-PCL amphiphilic triblock copolymer and paclitaxel at a mass ratio of 3:1 in chloroform, and add an equivalent amount of PCL-b-PEG-b-PCL amphiphilic Distearoylphosphatidylethanolamine-polyethylene glycol (2000) folic acid of triblock copolymer quality 1%, rotary evaporation removes chloroform to make solution form one layer uniform film on bottle wall, and nitrogen blows dry residual Chloroform, vacuum-dried until the chloroform is removed;

[0044] Add double-distilled water and the product of step (1) into a container so that the mass percentage of the product of step (1) is 1%, hydrate at 60°C for 12 hours, shake and mix, and ultrasonicate for 20 minutes in an ice bath to form a stable After the emulsion was filtered through membranes with a pore size of 0.45 μm and 0.22 μm in sequence, the filtrate was collected and freeze-dried fo...

Embodiment 2

[0059] A folic acid-targeted hydrophobic drug-loaded polymer vesicle is prepared by the following method:

[0060] (1) Dissolve the PCL-b-PEG-b-PCL amphiphilic triblock copolymer and hydroxycamptothecin with a mass ratio of 5:1 in dichloromethane, and add an equivalent amount of PCL-b-PEG-b-PCL Amphiphilic triblock copolymer quality 1% distearoylphosphatidylethanolamine-polyethylene glycol (2000) folic acid, evaporate and remove dichloromethane to make a uniform film, nitrogen blow dry residual dichloromethane, vacuum Dry until dichloromethane is removed;

[0061] (2) Add double-distilled water and the product of step (1) to a container so that the mass percentage of the product of step (1) is 2%, hydrate at 65°C for 4 hours, shake and mix, and ultrasonically in an ice bath After 15 minutes, a stable emulsion was formed. After filtering through membranes with pore sizes of 0.45 μm and 0.22 μm in turn, the filtrate was collected and freeze-dried for 30 hours to prepare a folic...

Embodiment 3

[0063] A folic acid-targeted hydrophobic drug-loaded polymer vesicle is prepared by the following method:

[0064] (1) Dissolve the PCL-b-PEG-b-PCL amphiphilic triblock copolymer and vincristine with a mass ratio of 2:1 in acetonitrile, and add an equivalent amount of PCL-b-PEG-b-PCL amphiphilic Distearoylphosphatidylethanolamine-polyethylene glycol (2000) folic acid of triblock copolymer quality 1%, rotary evaporation removes acetonitrile and forms a layer of uniform film on bottle wall, nitrogen blows dry remaining acetonitrile, vacuum-dries to Acetonitrile removal;

[0065] (2) Add phosphate buffered saline (PBS) and the product of step (1) in a container, make the mass percent of the product of step (1) be 8%, at 55 ℃, hydration 6h, shake and mix again, Stable emulsions were formed by ultrasonication in an ice bath for 10 minutes. After filtering through membranes with pore sizes of 0.45 μm and 0.22 μm in sequence, the filtrate was collected and freeze-dried for 18 hours ...

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Abstract

The invention discloses a folate-targeted hydrophobic medicine-loaded polymeric vesicle and a preparation method and use thereof. The polymeric vesicle is prepared by the following steps of: (1) dissolving amphiphilic triblock copolymer and a hydrophobic medicine in an organic solvent, adding distearamide phosphatidyl ethanolamine-polyethylene glycol (2000) folate, evaporating to remove the organic solvent to prepare a uniform thin film, blowing and drying; and (2) adding double distilled water and products in the step (1) into a container, hydrating, shaking and uniformly mixing to ultrasonically form stable emulsion, performing film filtering, collecting filter liquor and performing freeze drying, The polymeric vesicle has main advantages of liposome, nanoparticles and other particle medicine-loaded systems, stability in vivo and in vitro obviously superior to the liposome, thicker film layer, contribution to encapsulating the hydrophobic medicine, dual-targeting function of EPR passive targeting and folate active targeting, and capacity of making the medicine-loaded vesicle effectively targeted and gathered on a tumor part and fulfilling the aim of targeted therapy.

Description

technical field [0001] The invention relates to a targeted drug-loaded polymer vesicle, a preparation method and use thereof. Background technique [0002] Vesicles are supramolecular aggregates formed by the self-assembly of amphiphilic molecules. They are spherical single-chamber or multi-chamber association structures formed by closed bilayers, similar to cell membrane structures. As a drug carrier, vesicles have the characteristics of changing the distribution of drugs in the body, preventing drug degradation and inactivation, prolonging the action time of drugs, and reducing the toxicity and side effects of drugs. Compared with micelles, vesicles have the following characteristics: (1) vesicles have a large specific surface area and can absorb more reactants than micelles; (2) vesicle membranes composed of bilayer amphiphilic molecules That is, the bilayer membrane of the vesicle has strong rigidity, which can solubilize large drug molecules or enzymes; (3) The surface...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/34A61K47/22A61P35/00
Inventor 张琳华宋存先
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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