PH sensitive controllable nanometer particle carried with 5-Fu and its preparation method

A fluorouracil and drug-carrying nanotechnology, applied in the field of 5-fluorouracil-carrying nanoparticles, can solve the problems of bloody stool, poor recognition rate, short half-life and the like, and achieve the effects of easy storage, few toxic reagents, and large drug-carrying capacity.

Inactive Publication Date: 2006-12-20
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, it metabolizes quickly in the body and has a short half-life of only 5-10 minutes. Clinically, in order to achieve an effective blood drug concentration in the body, large doses, continuous administration or repeated administration are often used. The recognition rate of cells and diseased cells is poor, resulting in patients with loss of appetite, nausea, vomiting, stomatitis, gastritis, abdominal pain, diarrhea, and bloody stool in severe cases; bone marrow suppression is the main toxicity, manifested as leukopenia, thrombocytopenia and anemia ; Toxic side effects such as hair loss, nail changes, dermatitis, skin pigmentation increase

Method used

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  • PH sensitive controllable nanometer particle carried with 5-Fu and its preparation method
  • PH sensitive controllable nanometer particle carried with 5-Fu and its preparation method
  • PH sensitive controllable nanometer particle carried with 5-Fu and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] 1. Pullulan modification

[0017] Dissolve 2g of pullulan in 20ml of formamide solution, add 60ml of pyridine and 150ml of acetic anhydride into the solution, and react at 54°C for 48 hours. The resulting solution was reprecipitated in distilled water, washed and dried with methanol solution to obtain a white powder, that is, acetylated pullulan.

[0018] 2. Graft Sulfadetoxine

[0019] 2.1. Dissolve 5g of acetylated pullulan in 1,4-dioxane, and add 2.2g of succinic anhydride, 2.0g of dimethylaminopyridine, and 1.8g of triethylamine into the above solution, and then After reacting for 24 hours, the resulting solution was removed by a rotary evaporator to remove 1,4-dioxane, and 300 mL of carbon tetrachloride was used to remove unreacted succinic anhydride in the remaining liquid. The above solution was concentrated to 150 ml with a rotary evaporator, and then it was placed in diethyl ether at 4° C. for precipitation, and the resulting precipitate was vacuum-dried for ...

Embodiment 2

[0024] The acetylated pullulan and 5-fluorouracil prepared according to the first step method in Example 1 can be prepared according to the third step method in Example 1 to obtain the carrier 5 that has not been modified by the pH-sensitive group sulfidethoxine. - Fluorouracil nanoparticles, 20 mg of the above-mentioned drug-loaded nanoparticles were subjected to an in vitro release test at a temperature of 37° C. in a buffer solution of pH=6.0, 6.8, 7.4, and 8.2, and the release curve was as follows: figure 1 shown. Depend on figure 1 It can be seen that the total release of 5-fluorouracil at different pH values ​​is approximately the same, an average of 65% (18 hours), and there is no obvious pH sensitivity, but a certain sustained release effect has been achieved.

Embodiment 3

[0026] 20 mg of drug-loaded nanoparticles prepared according to the method of Example 1 were subjected to in vitro release tests in buffer solutions of pH=6.0, 6.8, 7.4, and 8.2 at a temperature of 37° C., and the release curves were as follows: figure 2 shown. Depend on figure 2 It can be seen that the total release of 5-fluorouracil suddenly increased from 62.92% of pH=8.2 and 69.94% of pH=7.4 to 80.72% of pH=6.8 and 83.12% of pH=6.0 in 18 hours, showing a strong pH sensitivity.

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Abstract

The invention discloses a pH-sensitive and controllable-release nanoparticle loaded with 5-fluorouracil drug and a preparation method thereof. The nanoparticle is a core-shell structure, its shell material is modified pullulan-sulfidethoxine, its core material is the acetyl part of modified pullulan, and the drug-loaded nanoparticle is at pH = Around 6.6-6.9, the drug is strongly aggregated and released, while the sustained release is realized and the particle size is maintained above pH=7.4, and the drug encapsulation rate is above 80%. The method comprises the steps of dissolving pullulan in formamide solution for hydrophobic modification, grafting sulfidethoxine into anhydrous 1,4-dioxane, and then making the prepared modified pullulan-sulfonamide Detoxine and 5-fluorouracil were dissolved in dimethyl sulfoxide and dialyzed to form drug-loaded nanoparticles. The invention has the advantages of improving the water solubility of 5-fluorouracil; by changing the grafting degree of sulfidethoxine and other conditions, it is easy to realize the controllable release of the drug at a specific pH value; the preparation process is simple, and it is an ideal carrier of 5-fluorouracil.

Description

technical field [0001] The invention relates to a pH-sensitive and controllable release nanoparticle loaded with 5-fluorouracil drug and a preparation method thereof, which belongs to the nanoparticle technology used for loading 5-fluorouracil. Background technique [0002] 5-Fluorouracil (5-Fluorouracil, abbreviated as 5-FU) is one of the earliest chemotherapeutic drugs, synthesized by Heidelberger in 1957. Has a lethal effect. It is mainly used clinically for breast cancer, colon cancer, rectal cancer, gastric cancer, liver cancer, ovarian cancer, cervical cancer, bladder cancer, prostate cancer and head and neck tumors. It is the first-line treatment drug for various malignant tumors and can also be used as radiation therapy sensitizers. Topical application can also treat basal cell carcinoma, and certain malignant skin diseases. However, it metabolizes quickly in the body and has a short half-life of only 5-10 minutes. Clinically, in order to...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/513A61K9/14A61K47/06A61P35/00
Inventor 刘亮张国亮张凤宝王淑兰
Owner TIANJIN UNIV
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