Lipid nano particle preparation containing composite formed fatty acid and anthracyclines antitumor antibiotics and preparation method thereof

A lipid nanoparticle and anti-tumor technology, which is applied in the field of medicine, can solve the problems of limiting the clinical use of liposome preparations, complicated liposome preparation process, and high industrial production costs, so as to improve drug encapsulation efficiency and drug loading capacity , Improve the encapsulation rate and drug loading capacity, and improve the effect of drug loading capacity

Active Publication Date: 2012-06-20
SICHUAN BAILI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] 2. The preparation process of liposome is complicated, and the cost of industrial production is relatively high, resulting in its price is also very expensive, for example: The price of liposomal preparations is as high as 1200 US dollars / support, and many patients cannot afford such expensive medical expenses, which greatly limits the clinical use of liposome preparations
[0016] In summary, it can be seen that there is no new preparation of anthracycline antitumor antibiotics with good stability, suitable for large-scale industrial production, simple preparation method, and low production cost.

Method used

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  • Lipid nano particle preparation containing composite formed fatty acid and anthracyclines antitumor antibiotics and preparation method thereof
  • Lipid nano particle preparation containing composite formed fatty acid and anthracyclines antitumor antibiotics and preparation method thereof

Examples

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Effect test

Embodiment 1

[0064] Take 10 mg of doxorubicin hydrochloride, dissolve it in 2 ml of water, add 50 mg / ml of NaHCO 3 40 μl of the solution was vortexed for one minute, 20 μl of oleic acid was added, vortexed until the water layer was colorless, centrifuged at 7000 r / min for 5 min, and the complex was precipitated. Take by weighing egg yolk lecithin (average molecular weight 800) 60mg, vitamin E 5mg, 60 μ l of soybean oil and complex are dissolved in ethyl acetate, sonication makes dissolution complete, organic solvent is evaporated to dryness under reduced pressure, adds 5% glucose solution 10ml, stirs, High-pressure milk homogenization 7 times to obtain doxorubicin oleic acid complex lipid nanoparticles. Particle size is 190nm, PDI is 0.125, see attached figure 1 .

Embodiment 2

[0066] Take 10mg of daunorubicin hydrochloride, dissolve it in 2ml of water, add 20μl of 10mg / ml NaOH solution, vortex for one minute, add 50μl of oleic acid and sonicate until the water layer is colorless, centrifuge at 7000r / min for 5min, and take the complex precipitate. Weigh 60 mg of soybean lecithin (average molecular weight 750), 5 mg of vitamin E, 40 μl of medium-chain fatty acid esters and the complex, dissolve them in ethanol, ultrasonically dissolve them completely, evaporate the organic solvent to dryness under reduced pressure, add 10 ml of normal saline, stir, and high-pressure milk Homogenize 7 times to obtain doxorubicin oleic acid complex lipid nanoparticles. The particle size is 175nm and the PDI is 0.210.

Embodiment 3

[0068] Take epirubicin hydrochloride 10mg, dissolve in 5ml water, add 20mg / ml Na 2 CO 3 30 μl of the solution was sonicated for 2 minutes, 70 μl of oleic acid was added and sonicated until the water layer was colorless, centrifuged at 7000 r / min for 5 minutes, and the complex was precipitated. Weigh 60 mg of soybean lecithin (average molecular weight 750), 40 mg of glyceryl monostearate and the complex are dissolved in methylene chloride, ultrasonically dissolve completely, evaporate the organic solvent to dryness under reduced pressure, add 10 ml of 5% glucose solution, and stir , and high-pressure milk homogenization 7 times to obtain epirubicin oleic acid complex lipid nanoparticles. The particle diameter is 267 nm, and the PDI is 0.257.

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Abstract

The invention provides a lipid nano particle preparation containing a composite formed fatty acid and anthracyclines antitumor antibiotics and a preparation method thereof. The lipid nano particle preparation comprises a composite formed by the anthracyclines antitumor antibiotics and fatty acid, and phospholipid and lipoid of lipid nano particle carrier ingredients, wherein the weight ratio of the composite, the phospholipid and the lipoid is 1:1-10:1-10:1-1000.

Description

technical field [0001] The invention relates to the technical field of medicine, and specifically provides an anthracycline antitumor antibiotic fatty acid complex lipid nanoparticle preparation and a preparation method thereof that can be widely used in industrial production. Background technique [0002] Anthracycline anti-tumor antibiotics are a class of broad-spectrum anti-tumor drugs commonly used in clinic. They can produce a wide range of biochemical effects on the body and have strong cytotoxicity. The main mechanism of action is that drug molecules intercalate into DNA and inhibit the synthesis of nucleic acids. Anthracycline antineoplastic antibiotics are widely used in the treatment of various cancers, such as leukemia, lymphoma, breast cancer, lung cancer, liver cancer and many other solid tumors. Such antineoplastic drugs mainly include: Doxorubicin (ADM), Daunorubicin (DNR), Epirubicin (Epirubicin, EPI), Pirarubicin (THP-ADM), Aclacinomycin (Aclacinomycin, ACM...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K9/19A61K31/704A61K47/48A61P35/00A61K47/12A61K47/14A61K47/24A61K47/44
Inventor 张凌龚照墉刘振谧
Owner SICHUAN BAILI PHARM CO LTD
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