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FA-mediated BBA/CM-beta-CD targeted drug delivery system as well as preparation method and application thereof

A FA-PEG-CM-, drug delivery system technology, applied in the field of medicine, can solve the problems of limiting the maximum allowable dose, drug concentration is not enough to achieve the effective concentration of tumor treatment, etc., to achieve the effect of enhancing drug efficacy

Inactive Publication Date: 2021-09-17
SOUTHWEST MEDICAL UNIVERISTY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, drug side effects also limit the maximum allowable dose, resulting in insufficient drug concentration to achieve effective therapeutic concentrations for tumors

Method used

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  • FA-mediated BBA/CM-beta-CD targeted drug delivery system as well as preparation method and application thereof
  • FA-mediated BBA/CM-beta-CD targeted drug delivery system as well as preparation method and application thereof
  • FA-mediated BBA/CM-beta-CD targeted drug delivery system as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1. Preparation of 2-butyryloxy-5-butyrylaminobenzoic acid (BBA)

[0040] 1. Synthesis of 2-hydroxy-5-butanamide benzoic acid

[0041] Weigh 0.4g (1.31mmol) of 5-aminosalicylic acid and place it in a 50mL single-neck round-bottomed flask, add 16mL of saturated sodium bicarbonate solution, stir and dissolve, and slowly add 0.27 g of butyryl chloride to the round-bottomed flask under an ice bath. 8 mL of acetone solution. After the dropwise addition was completed, the mixture was stirred magnetically and reacted at room temperature for 4h. TLC detected that the reaction was complete, the solvent was removed by rotary evaporation under reduced pressure, and the remaining liquid was cooled and acidified by adding 0.5 mL of hydrochloric acid. The solution was turbid, filtered with suction to obtain a light chocolate-colored precipitate, and finally dried in vacuum for 12 hours.

[0042] like image 3 shown, the 2-hydroxy-5-butyramide benzoic acid samples 1 H NMR a...

Embodiment 2

[0049] Example 2. Preparation of FA-modified 2-butyryloxy-5-butyrylaminobenzoic acid / carboxymethyl-β-cyclodextrin inclusion complex (BBA / FA-PEG-CM-β-CD) and Characterization

[0050]BBA / CM-β-CD inclusion complex has a good sustained release effect, which can improve drug efficacy and reduce toxic and side effects; however, it is difficult for BBA / CM-β-CD to pass through the plasma membrane of tumor cells, resulting in a low rate of uptake by target cells. . Therefore, in the present application, FA was selected to modify BBA / CM-β-CD to further increase the uptake rate of BBA / CM-β-CD by tumor cells.

[0051] The FA-mediated targeted drug delivery system can actively target the drug to the target organ or target cell, and realize the active targeted transportation of the folic acid-drug carrier conjugate, thereby improving the targeting of the drug and reducing the toxic and side effects of the drug. Compared with other ligands, FA has the advantages of high affinity to recept...

Embodiment 3

[0095] Example 3 In vitro study of inclusion compound

[0096] 1. Cell proliferation inhibition assay

[0097] (1) In this example, CaCo-2 cells (human cloned colon adenocarcinoma cells) and SW620 cells (human colon cancer cells) were used as model cells, and the MTT method was used to evaluate 5-ASA, NaB, 5-FU, BBA, FA- In vitro anticancer effects of PEG-CM-β-CD, BBA / CM-β-CD and BBA / FA-PEG-CM-β-CD. Take the cells in logarithmic growth phase and prepare a single cell suspension with 10% Gibco fetal bovine serum (FBS) and 1% penicillin-streptomycin in DMEM medium, and the cell concentration is 3.5×10 4 cells / mL, inoculate 100 μL of suspension in each well of a 96-well plate, set a blank cell control well, in 5% CO 2 Incubator overnight. Add PBS to the periphery of the 96-well plate to prevent excessive liquid evaporation during incubation.

[0098] (2) Discard the original medium, add different concentrations of BBA, FA-PEG-CM-β-CD, BBA / CM-β-CD, BBA / FA-PEG-CM-β-CD to the cu...

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to an FA-mediated BBA / CM-beta-CD targeted drug delivery system as well as a preparation method and application thereof. The carboxymethyl-beta-cyclodextrin inclusion compound targeted drug delivery system BBA / FA-PEG-CM-beta-CD which is modified by FA and carries BBA is successfully prepared, colon cancer can be inhibited, and the carboxymethyl-beta-cyclodextrin inclusion compound targeted drug delivery system has a definite targeting property on tumor parts; meanwhile, in-vivo action time is long, safety is high, and defects that butyric acid is poor in pharmacokinetic characteristic and narrow in safe dosage, and the BBA is poor in water solubility, low in bioavailability and the like can be effectively overcome. The discovery provides an extremely important new thought and a new method for clinical treatment of the colon cancer.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an FA-mediated BBA / CM-β-CD targeted drug delivery system, a preparation method and an application thereof. Background technique [0002] Colon cancer is a common malignant tumor of the digestive tract that occurs in the colon, which occurs at the junction of the rectum and the sigmoid colon. A domestic epidemiological data shows that the incidence of colon cancer has jumped to the fourth place, and the mortality rate ranks fifth. Colon cancer is mainly adenocarcinoma, mucinous adenocarcinoma, undifferentiated carcinoma, and its general shape is polypoid and ulcerative. The incidence of colon cancer is related to living habits, diet, genetic factors, inflammatory bowel disease and so on. In recent years, the incidence of colon cancer in my country has been increasing year by year, which seriously affects people's life and health. The treatment of colon cancer has be...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/222A61P35/00C07C233/54C07C231/12C07C231/02A61K47/54A61K47/60A61K47/69
CPCA61K31/222A61P35/00C07C233/54C07C231/12C07C231/02A61K47/545A61K47/60A61K47/6951
Inventor 钟志容刘中兵林燕陈林万钰洁陈振宇杜兴杰柏孝生
Owner SOUTHWEST MEDICAL UNIVERISTY
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