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Polymer lipid sphere carrying active drugs and preparation method thereof

A technology for active drugs and polymers, applied in the field of medicine, can solve the problems of difficulty in researching the relationship between microsphere particle size and drug efficacy, difficulty in screening particle size requirements, and inability to prepare particle size, etc., to ensure repeatability and size. Uniform and maintain the effect of drug activity

Inactive Publication Date: 2016-02-03
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the particle size and uniformity of the microspheres are also very important factors affecting the drug efficacy in vivo. However, the traditional methods cannot prepare microspheres with uniform particle size and controllability, and it is difficult to carry out the relationship between the particle size of the microspheres and the drug effect. Relationship research, it is difficult to screen the appropriate particle size requirements for different drugs and their different routes of administration

Method used

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  • Polymer lipid sphere carrying active drugs and preparation method thereof
  • Polymer lipid sphere carrying active drugs and preparation method thereof
  • Polymer lipid sphere carrying active drugs and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0070] A microporous membrane with a pore size of 9.2 μm is used to prepare PLGA microspheres loaded with hydrophilic proteins. The specific implementation method is as follows: figure 1 Shown: Accurately weigh 10 mg bovine serum albumin and dissolve it in 500 μL deionized water as the inner water phase (W 1 ); 160mgPLGA is added to 5mL dichloromethane solution and it is fully dissolved, as the oil phase (O); the aqueous solution that gets volume is 50mL containing 1%PVA as the external water phase (W 2 ). Add the inner water phase to the oil phase and homogeneously emulsify (20000rpm, 1min) to form water-in-oil (W 1 / O) type colostrum, then add the colostrum into the external water phase, mechanically stir (300rpm, 1min) to form W 1 / O / W 2 Type double milk. The double emulsion was poured into a rapid membrane emulsification reaction tank, and passed through the membrane 5 times under the action of nitrogen pressure of 0.1MPa to form an emulsion with uniform particle size....

Embodiment 2

[0072] A microporous membrane with a pore size of 9.2 μm is used to prepare polymer lipid spheres loaded with hydrophilic proteins. The specific implementation method is as follows figure 1 Shown: Accurately weigh 10 mg transferrin and dissolve in 500 μL deionized water as the inner water phase (W 1 ); 20mgHSPC (hydrogenated soybean lecithin) and 140mgPLGA were added to 5mL methylene chloride solution to make it fully dissolved, as the oil phase (O); the volume was 50mL containing 1%PVA aqueous solution as the external water phase (W 2 ). Add the inner water phase to the oil phase and homogeneously emulsify (20000rpm, 1min) to form water-in-oil (W 1 / O) type colostrum, then add the colostrum into the external water phase, mechanically stir (300rpm, 1min) to form W 1 / O / W 2 Type double milk. The double emulsion was poured into a rapid membrane emulsification reaction tank, and passed through the membrane 5 times under the action of nitrogen pressure of 0.1MPa to form an emu...

Embodiment 3

[0074] A microporous membrane with a pore size of 9.2 μm is used to prepare polymer lipid spheres loaded with hydrophilic proteins. The specific implementation method is as follows figure 1 Shown: Accurately weigh 10 mg of ovalbumin as the solid phase (S); add 40 mg of HSPC and 120 mg of PLGA to 5 mL of dichloromethane solution to fully dissolve it as the oil phase (O); take a volume of 100 mL containing 0.8% PVA aqueous solution as the external aqueous phase (W 2 ). Disperse the protein solid phase S in the oil phase, and homogeneously emulsify (20000rpm, 1min) to form a solid-in-oil (S / O) emulsion system, then add it to the external water phase, and mechanically stir (300rpm, 1min) , forming S / O / W2 double emulsion. The double emulsion was poured into a rapid membrane emulsification reaction tank, and passed through the membrane 4 times under the action of nitrogen pressure of 0.05MPa to form an emulsion with uniform particle size. It was mechanically stirred and solidified...

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Abstract

The invention relates to a polymer lipid sphere carrying active drugs and a preparation method thereof. The polymer lipid sphere comprises a hydrophobic skeleton and a phospholipid layer, wherein the hydrophobic skeleton consists of polymers; the phospholipid layer wraps the outside of the hydrophobic skeleton; hydrophobic tail ends of phospholipid molecules of the phospholipid layer are inlaid in the hydrophobic skeleton while hydrophilic head bases of the phospholipid molecules are exposed on the outer surface of the hydrophobic skeleton; the active drugs are buried in the hydrophobic skeleton; the average grain diameter of the polymer lipid sphere ranges from 0.1 micrometer to 30 micrometers; and the coefficient of dispersion is smaller than 0.1. The polymer lipid sphere is uniform in size, controllable, high in embedding rate, high in activity, low in burst release and stable in drug release, carries the active drugs, is long-acting, releases the drugs in a sustained or controlled mode, is degradable, and has a multi-cavity or core-shell structure, and M cells can take in the polymer lipid sphere quickly, so that translocation amount and translocation efficiency of the drugs or vaccines through the M cells are improved.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to a polymer lipid ball loaded with active drugs and a preparation method thereof, which can be used for loading active drugs such as proteins, polypeptides or vaccines. Background technique [0002] In recent years, with the rapid development of biotechnology and genetic engineering, a large number of biologically active drugs such as proteins, peptides, and vaccines have flourished, and more and more drugs have been used clinically. Bioactive drug molecules are relatively fragile and susceptible to various physical and chemical factors, resulting in short circulation half-life and low bioavailability. At present, most bioactive drugs are administered through parenteral routes, which usually require repeated injections to prolong the curative effect, resulting in Patient compliance is poor. [0003] In order to prolong the circulating half-life of biologically active drugs in the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/24A61K47/34A61K47/12A61K47/18
Inventor 马光辉王连艳苏志国杨婷媛马童童周炜清
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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