A pH-sensitive fe3o4@ldh-loaded nano drug particle of methotrexate, its preparation method and its application

A technology of methotrexate and nano-drugs, which is applied in the direction of drug combinations, pharmaceutical formulas, and medical preparations of non-active ingredients, etc. It can solve the problems of poor actual targeting performance, inability to effectively act on lesion sites, lack of identification of lesion sites, etc. problems, to achieve the effect of improving efficacy and bioavailability, increasing drug loading, and good water solubility

CN106552269BActive Publication Date: 2019-04-16NANJING UNIV OF SCI & TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Publication Date
2019-04-16

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Abstract

The invention discloses pH sensitive-type Fe3O4 coated LDH methotrexate-loaded nano drug particles. According to the invention, LDH is directly added in a preparation system of Fe3O4 nanoparticles, while the Fe3O4 nanoparticles are formed, at the same time, the surface of the Fe3O4 nanoparticles is coated with LDH through a self-assembling mode, a Fe3O4 coated LDH carrier is formed, and MTX can effectively loaded on the Fe3O4 coated LDH carrier through a subject and object exchange technology. The employed LDH can increase the biocompatibility of the Fe3O4 nanoparticles, and a special structure of LDH can greatly increase the load capacity of an anticancer medicine. The prepared Fe3O4 coated LDH-MTX has excellent medicine slow release performance, has obvious inhibition effect on tumor cells, has good antineoplastic effect, and has large application potential in the field of targeting tumour treatment.
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Description

technical field

[0001] The present invention relates to a kind of pH sensitive Fe 3 o 4 @LDH Nano drug particles loaded with methotrexate, its preparation method and its application belong to the field of nano medicine technology. Background technique

[0002] Methotrexate (MTX) is one of the well-known antitumor drugs, which can treat malignant tumors such as head and neck cancer, breast cancer, skin cancer, and lung cancer. Unfortunately, MTX has a very short plasma half-life and high efflux rate compared to the influx rate, necessitating high doses of MTX for treatment. In addition, the dose of drugs applied to the organism does not fully reach the tumor site, but spreads throughout the body, causing toxic side effects on normal tissues, which limits its clinical application. Delivering anti-tumor drugs to the lesion site through nano-carriers, adjusting drug release according to the nature and strength of a certain stimulus-sensitive signal in the external environment...

Examples

Embodiment 1

[0031] Example 1: Fe 3 o 4 Preparation of @LDH-MTX

[0032] Sequentially weigh 0.5g FeCl 3 ·6H 2 O, 3.0g sodium acetate, dissolved in 40mL ethylene glycol, ultrasonically stirred for 20min to disperse the system evenly, then added 2.0g LDH to the mixed solution, continued ultrasonically stirred for 10min, then transferred the uniform mixed solution into polytetrafluoroethylene In the reaction kettle, react at 200°C for 10h. After the reaction was completed, the product was poured out, extracted by magnetic decantation, and washed several times with deionized water. The washed product was dried in a vacuum oven at 25°C to obtain dry powdered Fe 3 o 4 @LDH Carrier.

[0033] Sequentially weigh 50 mg of dry Fe 3 o 4 @LDH, 2.5mg MTX, dissolved in 20mL deionized water, ultrasonicated for 5min to disperse the system evenly. Then transfer to a one-necked flask, and react in the dark at 55°C for 3 days.

[0034]After the reaction was completed, the product was poured out, ex...

Embodiment 2

[0037] Example 2: Fe 3 o 4 Preparation of @LDH-MTX

[0038] Sequentially weigh 0.5g FeCl 3 ·6H 2 O. Dissolve 3.0g of sodium acetate in 40mL of ethylene glycol, stir ultrasonically for 20min to disperse the system evenly, then add 2.0g LDH to the mixture, and continue ultrasonically stirring for 10min. Afterwards, the homogeneous mixed liquid was transferred into a polytetrafluoroethylene reactor and reacted at 200°C for 8 hours. After the reaction was completed, the product was poured out, extracted by magnetic decantation, and washed several times with deionized water. Then, the product was dried in a vacuum oven at 25°C to obtain dry powdered Fe 3 o 4 @LDH Carrier.

[0039] Sequentially weigh 50 mg of dry Fe 3 o 4 @LDH, 3mg MTX, dissolved in 20mL deionized water, ultrasonicated for 5min to disperse the system evenly. Then transfer to a one-necked flask, and react in the dark at 55°C for 3 days.

[0040] After the reaction was completed, the product was poured out,...

Embodiment 3

[0041] Example 3: Fe 3 o 4 Preparation of @LDH-MTX

[0042] Sequentially weigh 0.5g FeCl 3 ·6H 2 O. Dissolve 3.0g of sodium acetate in 40mL of ethylene glycol, and stir ultrasonically for 20min to disperse the system evenly. Then, 2.0 g LDH was added to the mixture, and ultrasonic stirring was continued for 10 min. Afterwards, the homogeneous mixed liquid was transferred into a polytetrafluoroethylene reactor, and reacted at 190° C. for 10 h. After the reaction was completed, the product was poured out, extracted by magnetic decantation, and washed several times with deionized water. Then, the product was dried in a vacuum oven at 30°C to obtain dry powdered Fe 3 o 4 @LDH Carrier.

[0043] Sequentially weigh 50 mg of dry Fe 3 o 4 @LDH, 5mg MTX, dissolved in 20mL deionized water, ultrasonic 5min to make the system evenly dispersed. Afterwards, it was transferred to a one-necked flask, and reacted in the dark at 65° C. for 3 days.

[0044] After the reaction was comp...