PCL-b-PEG-b-PCL carried hydrophobic medicine polymer vesica as well as preparation method and application thereof

A hydrophobic drug, pcl-b-peg-b-pcl technology, applied in the direction of drug combination, pharmaceutical formula, capsule delivery, etc., can solve the problems of unsatisfactory treatment effect, large toxic and side effects, etc., and achieve strong permeability and stability Good performance and prolong cycle time

Inactive Publication Date: 2011-01-12
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

[0007] 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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  • PCL-b-PEG-b-PCL carried hydrophobic medicine polymer vesica as well as preparation method and application thereof
  • PCL-b-PEG-b-PCL carried hydrophobic medicine polymer vesica as well as preparation method and application thereof
  • PCL-b-PEG-b-PCL carried hydrophobic medicine polymer vesica as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] A PCL-b-PEG-b-PCL-loaded hydrophobic drug polymer vesicle is prepared by the following method:

[0041] (1) Dissolve the PCL-b-PEG-b-PCL amphiphilic triblock copolymer and paclitaxel with a mass ratio of 3:1 in chloroform, and remove the chloroform by rotary evaporation to form a chloroform on the bottle wall. Layer uniform film, blow dry the residual chloroform with nitrogen, and vacuum dry until the chloroform is removed;

[0042] (2) 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, then shake and mix, and ultrasonically in an ice bath After 20 min, a stable emulsion was formed, filtered through membranes with a pore size of 0.45 μm and 0.22 μm successively, and the filtrate was collected and freeze-dried for 20 h to prepare a PCL-b-PEG-b-PCL-loaded paclitaxel polymer vesicle (see figure 1 ).

Embodiment 2

[0044] A PCL-b-PEG-b-PCL-loaded hydrophobic drug polymer vesicle is prepared by the following method:

[0045] (1) Dissolve the PCL-b-PEG-b-PCL amphiphilic triblock copolymer and hydroxycamptothecin with a mass ratio of 5:1 in methylene chloride, remove methylene chloride by evaporation and make a uniform film , dry the residual dichloromethane with nitrogen, and vacuum-dry until the dichloromethane is removed;

[0046] (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, filtered through membranes with a pore size of 0.45 μm and 0.22 μm in turn, and the filtrate was collected and freeze-dried for 30 hours to prepare a PCL-b-PEG-b-PCL-loaded hydroxycamptothecin polymersome.

Embodiment 3

[0048] A PCL-b-PEG-b-PCL-loaded hydrophobic drug polymer vesicle is prepared by the following method:

[0049] (1) Dissolve mass ratio 2: 1 PCL-b-PEG-b-PCL amphiphilic triblock copolymer and vincristine in acetonitrile, remove acetonitrile by rotary evaporation to form a uniform film on the bottle wall, Dry residual acetonitrile with nitrogen, and vacuum-dry until the acetonitrile is removed;

[0050] (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, Ultrasound in ice bath for 10 minutes to form a stable emulsion, after filtering through membranes with a pore size of 0.45 μm and 0.22 μm in sequence, the filtrate was collected and freeze-dried for 18 hours to prepare a PCL-b-PEG-b-PCL-loaded vincristine polymer Vesicles.

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Abstract

The invention discloses a PCL-b-PEG-b-PCL carried hydrophobic medicine polymer vesica as well as a preparation method and application thereof. The polymer vesica is manufactured by the following steps of: (1) dissolving amphipathy triblock copolymer and hydrophobic medicine in organic solvent, evaporating to remove the organic solvent to prepare film, blowing and drying; and (2) adding double distilled water and the product in the step (1) in a container, hydrating, evenly mixing through oscillation, performing ultrasonic to form stable emulsion, collecting filtrate and freezing after filtering the film. The vesica has the main advantages of particle medicine carrying systems such as liposome and nanometer; the stability inside and outside the polymer vesica is remarkably superior to the liposome; the film layer is thicker and is beneficial to packaging hydrophobicity medicine; in the preparation process, emulsifier or surface active agent is not needed, thereby overcoming the defect that the a great amount of emulsifier or surface active agent is needed for traditionally preparing a medicine release system and avoiding toxic side effect to the organism caused by using reagent.

Description

technical field [0001] The invention relates to an amphiphilic block copolymer drug-loaded polymer vesicle and its preparation method and application 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 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K9/50A61K31/475A61K31/09A61K31/337A61K31/4745A61P35/00
Inventor 张琳华宋存先
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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