Lipid-based drug of serum degradable carrier and application method of lipid-based drug

A degradable, serum-based technology, applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as variable configuration, high-level configuration disturbance, and loss of recognition ability. Achieve the effects of low immune response of blood cells, high mechanical strength and improved efficiency

Inactive Publication Date: 2013-02-06
LULIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, when used to encapsulate polar drugs, the cryptic epitope antigen of PC loses its ability to recognize, thereby inhibiting the "phagocytosis" of immune cells to clear apoptotic cells; Kinetics and pharmacodynamics are greatly affected, and drug stability is not high; the mechanical strength of PC is not ideal, and the disturbance of its advanced configuration is obvious when it is used for the encapsulation of biopharmaceuticals

Method used

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  • Lipid-based drug of serum degradable carrier and application method of lipid-based drug
  • Lipid-based drug of serum degradable carrier and application method of lipid-based drug
  • Lipid-based drug of serum degradable carrier and application method of lipid-based drug

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Zr(EPC) 2 Nanocarriers degrade in serum:

[0037] Accurately weigh 160 μg of dry carrier, add 1.5 ml of fresh serum, and stir at 3000 rpm / min for 20 min at 4 °C to obtain a translucent suspension dispersion, which is then shaken and degraded in a constant temperature oscillator at 37 °C; 3, 5, 7, 9, 10, 11, 11.5, 12, 12.5, 13 h Use a micropipette to draw 100 μl of degradation solution, centrifuge at 16000 rpm / min for 20 min at high speed; pipette 70 μl of supernatant in 1 ml colorimetric tube, dilute to 400 μl with distilled water, then add 200 μl ascorbic acid (100 g / l), 400 μl ammonium molybdate color solution (13 g ammonium molybdate + 0.35 g antimony potassium tartrate + 150 ml H 2 SO 4 500 ml); after 15 min of color development, the absorbance was measured at 700 nm, using serum samples as a reference.

[0038] The degradation rate of the carrier (%) = (the phosphorus mass of the supernatant ÷ the total phosphorus mass of the carrier) × 100 %.

[0039] Such as ...

Embodiment 2

[0041] Zr(SPC) 2 Nanocarriers degrade in serum:

[0042] Add 160 μg of dry carrier into a centrifuge tube (2 ml) of 1.5 ml of fresh serum, stir at a high speed (3000 rpm / min) at 4°C, and turn into a translucent suspension dispersion after 20 min; place the centrifuge tube in 37°C constant temperature shaker, shake the degradation carrier; pipette 100 μl degradation solution at 3, 5, 7, 9, 11, 12, 13, 14, 15, 15.5, and 16 h respectively, and centrifuge at a high speed (16000 rpm / min) for 20 min; pipette 70 μl of the supernatant into a 1 ml colorimetric tube, dilute to a volume of 400 μl, add 200 μl of ascorbic acid (100 g / l), 400 μl of ammonium molybdate chromogenic solution (13 g ammonium molybdate + 0.35 g antimony potassium tartrate + 150 ml H 2 SO 4 500 ml), develop color for 15 min; measure the absorbance at 700 nm with reference to the serum sample, and calculate the mass of phosphorus and the degradation rate of the carrier. The degradation rate of the carrier (%) = ...

Embodiment 3

[0045] A serum-degradable lipid drug, comprising liposome and serum, wherein the liposome is formed by encapsulating the drug with lecithin zirconium nanoparticles, and the dosage ratio of liposome and serum is 187 μg: 1.5 mL. Lecithin zirconium nanoparticles are egg yolk phospholipid zirconium Zr (EPC) 2 , the drug is the ribosome inhibitory protein bitter melon MAP30.

[0046] The above-mentioned method of using the lipid drug of the serum-degradable carrier is to inject the carrier or the liposome drug into the serum in vitro.

[0047] Zr(EPC) 2 – Drug release from MAP30 liposomes:

[0048] Liposomes were prepared by the following process, protein:carrier (mass ratio) 0.34:1, pH 8.52 (10 mM PBS+100 mM NaCl), reaction time 15 h; liposomes were centrifuged, washed and freeze-dried, wherein MAP30 The content (mass ratio) is 24.0 ± 1.0 %; in 187 μg of liposomes, inject 1.5 ml of fresh in vitro serum samples, stir at 3000 rpm / min for 20 min (4°C), and obtain a translucent sus...

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Abstract

The invention discloses a lipid-based drug of a serum degradable carrier and an application method of the lipid-based drug, and belongs to the technical field of pharmacy. The lipid-based drug of the serum degradable carrier is characterized by comprising a liposome and serum, the liposome is formed by coating the drug with lecithin zirconium nanometer particles, dosage ratio of the liposome and the serum is 184-191 microgram: 1.5mL, and the application method is that the carrier or the lipid-based drug is externally injected into the serum. Pressure in terms of acidity, salinity and oxidation metabolite is not caused to blood cells by a degradation product, efficiency of directional delivery and target recognition of the drug to recipient cells can be improved, the lipid-based drug has the advantages of high mechanical strength and stability of drug coating conformation, and can be widely applied for developing slow-release drugs with a low blood cell immune response and no residual and for preparing a novel formulation with controlled release and efficient delivery of ribosome profilin.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and relates to a serum-degradable carrier lipid drug and a use method thereof. Background technique [0002] In the plasma membrane of eukaryotic cells and mammalian cells, lecithin (phosphatidylcholine, PC) is the most widely distributed lipid. Soy lecithin (SPC) and egg yolk lecithin (EPC) are the most common PC products, in sn –1–site and sn The substituents at the -2- position are saturated acyl groups and unsaturated fatty acid carbon chains (the degree of unsaturation is equal to 2). In the PC molecule, the carbon chain of the fatty acid is not branched, and the unsaturated bond belongs to the cis configuration, which has a great influence on the fluidity. Phospholipids are distributed asymmetrically in the plasma membrane, and the outer microdomain is mainly composed of PC. [0003] Active phospholipases C and D selectively synthesize PC, which is used to perform the clearance of apop...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/46A61K47/24A61K38/16A61K45/00
Inventor 薛金辉乔元彪霍宇平郭彩珍翟言强卫英慧李彦威
Owner LULIANG UNIV
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