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Targeted anti-bladder-cancer albumin carrying mitomycin drug and preparation method thereof

A technology containing mitomycin and mitomycin, which can be used in antitumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of high toxicity and low therapeutic index, and achieve prolonged action time, reduced side effects, and selectivity. strong effect

Inactive Publication Date: 2013-04-17
李云龙 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Mitomycin is a cell cycle non-specific drug with a broad anti-tumor spectrum and rapid action, but its therapeutic index is not high and its toxicity is high

Method used

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  • Targeted anti-bladder-cancer albumin carrying mitomycin drug and preparation method thereof
  • Targeted anti-bladder-cancer albumin carrying mitomycin drug and preparation method thereof
  • Targeted anti-bladder-cancer albumin carrying mitomycin drug and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027] The preparation of the targeted anti-bladder cancer albumin-loaded mitomycin drug of the present invention comprises the following steps:

[0028] a. Preparation of albumin-loaded mitomycin (MMC-NS) nanospheres:

[0029] (a1) Dissolve bovine serum albumin with normal saline, and prepare bovine serum albumin solution containing 0.15g per milliliter; dissolve mitomycin with bovine serum albumin solution, and prepare MMC bovine serum albumin containing 0.06mg MMC per milliliter protein solution;

[0030] (a2) Put 100ml of cyclohexane, 3.0mlspan40 and 0.5ml of MMC bovine serum albumin solution into a three-neck flask, stir well with a stirrer; ultrasonic emulsification with a power of 200W for 15min, add 2ml of glutaraldehyde saturated toluene solution, 20°C Stir and react for 2 hours, put the material into a centrifuge, centrifuge at a speed of 2000r / min for 2min, discard the deposited large microspheres, and then centrifuge at a speed of 500r / min for 3min to obtain the r...

Embodiment 2

[0038] The steps are the same as those in Example 1, except that the physiological saline in step (a1) is configured to a protein concentration of 0.20 g / ml, and is configured as MMC bovine albumin solution containing 0.07 mg MMC per ml; the emulsifier in step (a2) is modified. is 3.6ml span80, ultrasonic power is 300W, 3000r / min down to large microspheres, 600r / min to get the required nano-microspheres; (b1) step contains MMC-NS 2.5mg per ml; c step is changed to 6 ℃ After stirring for 18h, the centrifugal speed was 12000r / min, and the time was 10min, to obtain the doublet drug BDI-1-MMC-NS with uniform size and good dispersibility.

Embodiment 3

[0040] The steps are the same as those in Example 1, except that the physiological saline in step (a1) is configured to a protein concentration of 0.30 g / ml, and is configured as MMC bovine albumin solution containing 0.08 mg MMC per ml; the emulsifier in step (a2) is modified. It is 4.0ml span83, the power of ultrasonic wave is 400W, the large microspheres are lowered at 2000r / min, and the required nano-microspheres are obtained at 600r / min; (b1) step contains 2.5mg of MMC-NS per ml; step c is changed to 6 ℃ After stirring for 18h, the centrifugal speed was 10000r / min, and the time was 15min, the doublet drug BDI-1-MMC-NS with uniform size and good dispersibility was obtained.

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Abstract

The invention discloses a targeted anti-bladder-cancer albumin carrying mitomycin drug and a preparation method thereof. The targeted anti-bladder-cancer albumin carrying mitomycin drug is characterized in that drug molecules contain albumin molecules, anti-human-bladder-cancer monoclonal antibodies (BDI-1) and mitomycin (MMC), and the synthetic method of the drug molecules comprises the following steps: using glutaraldehyde as a cross-linking curing agent, and combining mitomycin molecules with bovine blood albumin molecules to be prepared into albumin carrying mitomycin (MMC-NS) nanoparticles with the particle size being 280-350 nanometer; then using a heterogenic bifunctional coupling agent N-succinimido-3-(2-pyridyl disulfide) propionate (SPDP) to causes the albumin carrying mitomycin molecules to be coupled with a pyridyl disulfide group (PDP) to obtain MMC-NS-PDP molecules; and finally, causing MMC-NS-PDP to reacting with BDI-1-SH molecules to obtain the drug with the molecules containing anti-human-bladder-cancer antibodies, the albumin molecules and the mitomycin, namely the targeted anti-bladder-cancer albumin carrying mitomycin drug, (BDI-1-MMC-NS for short). The drug has strong targeting to bladder cancer, a strong curative effect on bladder cancer, and a smaller influence on normal tissue cells.

Description

technical field [0001] The present invention relates to a targeted anti-bladder cancer albumin-loaded mitomycin drug and a preparation method thereof, in particular to a drug containing anti-human bladder cancer monoclonal antibody, albumin and mitomycin in its molecule and its preparation method. Preparation. Background technique [0002] Bladder cancer is one of the most common malignant tumors in humans, which seriously threatens people's life and health. More than 90% of them are urothelial carcinoma (transitional cell carcinoma, TCC), and about 10% of them eventually develop into Muscle-invasive or metastatic bladder cancer has poor long-term efficacy. Due to its high incidence and recurrence rate, intravesical chemotherapy is one of the main treatment methods for non-muscle-invasive bladder cancer. Currently, intravesical infusion chemotherapy drugs include mitomycin (MMC for short), camptothecin, pirapiricin, epirubicin, and daunorubicin. One of the reasons for the ...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/42A61K31/407A61P35/00
Inventor 李云龙周红华
Owner 李云龙
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