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Vincristine lipid microbubble and preparation method thereof

A technology of vincristine and lipid microbubbles, which is applied in the directions of liposome delivery, pharmaceutical formulations, and medical preparations of inactive ingredients, etc., can solve the problems of low drug concentration, rare research, and low drug loading capacity. , to achieve the effect of reducing degradation, enhancing immune function and simple preparation process

Inactive Publication Date: 2015-03-04
唐春林
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although the research on microbubbles in contrast agents is becoming more and more mature, it is rare to study microbubbles as a new type of drug carrier
Although microbubbles have unique advantages in targeted drug delivery and promotion of drug absorption at the target site, there are many technical difficulties that cannot be overcome at present: for example, as a drug carrier, the drug loading capacity of microbubbles is low, resulting in the delivery to the target site. The concentration of the drug is low, which is not enough for the drug to produce effective pharmacological effects, etc.

Method used

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  • Vincristine lipid microbubble and preparation method thereof
  • Vincristine lipid microbubble and preparation method thereof
  • Vincristine lipid microbubble and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] 1), preparation of lecithin mixture

[0067] Egg yolk lecithin: glycerol: phosphate buffer solution is mixed uniformly at a ratio of 6:58:100, calculated by mass percentage.

[0068] 2), preparation of vincristine albumin nanoparticles

[0069] Adopt desolvation method to prepare vincristine albumin nanoparticles, accurately weigh 20mg bovine serum albumin and dissolve it in 2mL water, and take another 50mg vincristine and dissolve it in 12mL absolute ethanol, with a volume flow rate of 1mL / min Add vincristine ethanol solution dropwise to albumin aqueous solution, add 100mL glutaraldehyde with a concentration of 0.25%, and stir for 4 hours in the dark to solidify, and remove ethanol by rotary evaporation at 35°C to obtain vincristine albumin nanoparticle suspension , see the result figure 1 . The encapsulation efficiency was 88.48% as measured by centrifugation.

[0070] 3) Preparation of vincristine-loaded albumin nanoparticles and lipid microbubbles

[0071] Take...

Embodiment 2-10

[0082] Examples 2-10 are operated according to the following parameters, and the others are the same as in Example 1, and the cumulative release rate experiment is detected under the condition of adding ultrasound.

[0083]

[0084]

[0085] Examples 8-10 of the present invention are comparative examples. Experimental results show that the type of phospholipids, the ratio of phospholipids, glycerol and phosphate buffer, and the selection of glutaraldehyde have a very important impact on the present invention.

[0086] The experimental results of Examples 1-7 of the present invention show that: through the cooperation of various parameters of the present invention, the encapsulation efficiency can be realized at 82.3% to 92%, and the obtained vincristine-loaded albumin lipid microbubbles have a diameter of 4 to 7 Micron, in vitro and in vivo imaging effects are good, and the 24h in vivo drug release rate is 80-92%, which has a good application prospect.

Embodiment 11

[0088] The vincristine lipid microbubble that embodiment 1 is made is made freeze-dried powder injection preparation

[0089] Pre-freezing: Put the subpackaged vincristine lipid microbubbles on the inner partition of the freeze-drying box. In the manual interface, set the temperature of the plate layer to 0°C for 1 minute (turn on the electric heating). After entering the box, Keep the product below 1°C for 60 minutes; turn on the two compressors, set the plate temperature to -40°C for 1 minute, and keep the product below -35°C for 60 minutes; set the plate temperature to -11°C for 60 minutes, and wait for the product to reach -11°C , Keep the product at -11°C for 60min; set the plate temperature at -38°C for 1min, keep the product at -35°C for 60min.

[0090] - Secondary drying (sublimation drying)

[0091] Refrigerate the back box, and when the temperature of the back box reaches -40°C, turn on the vacuum pump, and then open the small butterfly valve after 2 seconds to evac...

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Abstract

The invention provides a vincristine lipid microbubble. The vincristine lipid microbubble comprises a lipid bilayer membrane, gas, albumin nanoparticles for carrying vincristine; and the gas and the albumin nanoparticles for carrying the vincristine are wrapped by the lipid bilayer membrane. The vincristine lipid microbubble has the higher medicine loading capacity and the higher encapsulation efficiency; the blood concentration of target positions can be improved; the action time of medicines at the target positions is prolonged; the medicine degradation is reduced; and the medicine stability is improved. In addition, the nanoparticles have the beneficial effects that the selective distribution of the medicines is promoted; the medicines are better transmitted to enter lesion tissues; the pesticide effect can be improved; and the toxic and side effects can be reduced. The invention further discloses a preparation method of the vincristine lipid microbubble. The preparation process is simple; industrialization is easily achieved; the preparation process does not relate to chemical reactions; organic solvents with high toxicity are not adopted; the safety performance is high; and the environment friendliness is high.

Description

technical field [0001] The invention relates to vincristine, in particular to vincristine lipid microbubbles and a preparation method thereof. Background technique [0002] Vincristine is an alkaloid extracted from periwinkle. It is an anticancer drug that interferes with protein synthesis. It is mainly effective for lymphoma, choriocarcinoma and testicular tumor, and it is also effective for lung cancer, breast cancer and monocytic leukemia. However, vincristine is sensitive to light, unstable to heat, and has neurotoxicity, dyskinesia, bone marrow suppression, and gastrointestinal reactions. Existing vincristines all have problems such as short drug target action time, insufficient drug stability, and fast drug degradation speed. [0003] Finding drug carriers with high efficiency, low toxicity and good biocompatibility is the key to targeted drug delivery. The development trend of targeted drug delivery system is to use liposomes, microspheres, etc. as drug carriers, am...

Claims

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Application Information

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IPC IPC(8): A61K31/475A61K49/22A61K9/00A61K47/24A61P35/00
CPCA61K9/0019A61K9/127A61K9/19A61K31/475A61K47/24A61K47/42
Inventor 唐春林刘泽英高耀华
Owner 唐春林
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