Miboplatin liposome and preparation method thereof

A liposome and miplatin technology, applied in the field of medicine, can solve the problems of lack of specificity and selectivity, toxic and side effects of cancer cells, and achieve the effects of drug stability, delayed release, and avoidance of leakage

Inactive Publication Date: 2014-04-23
SHANGHAI NEW ASIA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] However, platinum-based anticancer drugs are cytotoxic compounds that lack specificity and selectivity for cancer cells. While killing cancer

Method used

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  • Miboplatin liposome and preparation method thereof
  • Miboplatin liposome and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Preparation of miplatin liposomes by film dispersion method: firstly mix 2.5 mL of chloroform and ethanol at a volume ratio of 9:1 as an organic solvent for later use, then weigh lecithin (700 mg), cholesterol (100 mg) and miplatin (70 mg ), add the organic solvent to dissolve, put the solution in a round bottom flask and rotate it to dryness under reduced pressure to form a phospholipid film, then add 100 mL of phosphate buffer solution to the round bottom flask, fully shake the flask to hydrate for 10- After 20 minutes, the lipid film was hydrated and fell off, the liposome liquid was taken out in a beaker, placed on a magnetic stirrer, stirred for 30-60 minutes, mixed evenly, and then sized through a 0.8 μm microporous membrane to obtain the final product. The particle size of miplatin liposomes prepared by this method is 270 ± 14 nm, and the encapsulation efficiency is about 62.9%.

Embodiment 2

[0034]Preparation of miplatin liposomes by film dispersion method: weigh dipalmitoylphosphatidylcholine (600 mg), cholesterol (100 mg) and miplatin (70 mg), add 3 mL of chloroform to dissolve, and place the solution in a circular Rotate the bottom flask and evaporate to dryness under reduced pressure to form a phospholipid film, add 80 mL of phosphate buffer solution to the flask, shake the flask fully for 10-20 min to hydrate the lipid film, and take out the liposome liquid in a beaker , placed on a magnetic stirrer, stirred for 30-60 min, mixed evenly, and sized through a 0.8 μm microporous membrane. The particle size of miplatin liposomes prepared by this method is 190 ± 10 nm, and the encapsulation efficiency is about 77.4%.

Embodiment 3

[0036] Preparation of miplatin liposomes by injection method: first mix 2.5 mL of chloroform and ethanol at a volume ratio of 9:1 as an organic solvent for later use, then weigh lecithin (700 mg), cholesterol (100 mg) and miplatin (70 mg ), added to the organic solvent to dissolve, and then injected the oil phase solution into 100 mL of sodium succinate buffer at a uniform speed using a syringe, stirred to remove the organic solvent, then milked evenly, and sized through a 0.8 μm microporous membrane, Promptly obtain miplatin liposome. The particle size of the liposome is 220 ± 18 nm, and the encapsulation efficiency can reach 70.8%.

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Abstract

The invention relates to a miboplatin liposome and a preparation method thereof. A fat-soluble metal complex miboplatin is encapsulated in a liposome, has targeting property to tumor cells when serving as an anti-tumor preparation, can be used for effectively reducing medicine toxicity and improving medicine stability, and is advantageous to transport and store. The miboplatin liposome is prepared from miboplatin, phospholipid, cholesterol, organic solvent and buffer solution system, wherein miboplatin, phospholipid and cholesterol are dissolved in the organic solvent according to the prescribed amount to obtain an oil phase; the buffer solution system is used as an aqueous phase, and the volume ratio of the oil phase to the aqueous phase is (1:20)-(1:60). The preparation method comprises a film dispersion method, an injection method, an ultrasonic dispersion method, a lyophilization method and the like, wherein a miboplatin liposome precursor is prepared by the lyophilization method, so that medicine leakage, particle aggregation and oxidation and hydrolysis of phospholipid in liquid state can be avoided. The average particle diameter of the miboplatin liposome prepared by the method can be below 150nm, the encapsulation efficiency is 50-95 percent, and a new thought is provided to research of novel anti-tumor preparations.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a miplatin liposome for treating cancer and a preparation method thereof. Background technique [0002] Platinum anticancer drugs, as a member of anticancer drugs, have been widely used in cancer chemotherapy. Following the success of the first-generation platinum drug cisplatin and the second-generation platinum drug carboplatin, there have been the third-generation platinum drug oxaliplatin and the new-generation neda Platinum (nedaplatin), Shu Platinum (sunplatin) and lobaplatin (lobaplatin) approved for marketing. Cisplatin is recommended as the drug of choice in 18 cancers including esophageal cancer and non-small cell lung cancer; carboplatin is not only the drug of choice for 5 cancers including non-small cell lung cancer and hepatoblastoma, it can also be used as a drug for bladder cancer, The second-choice treatment drug for 8 cancers including cervical cancer; Oxalip...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/282A61K9/19A61P35/00A61J3/00
Inventor 张晓航黄琳凤戴杰
Owner SHANGHAI NEW ASIA PHARMA
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