A kind of effervescent drug producing polylactic acid glycolic acid and its preparation method and application

A technology of lactic acid glycolic acid and glycolic acid, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve problems such as poor tumor effect, achieve good blood compatibility and biocompatibility, high drug utilization rate, low cost effect

Inactive Publication Date: 2018-08-28
UNIV OF SHANGHAI FOR SCI & TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the above-mentioned technical problems in the prior art, the present invention provides a poly(lactic-co-glycolic acid) effervescent drug and its preparation method and application. It solves the technical problem of the poor effect of using high-intensity focused ultrasound to treat tumors in the prior art

Method used

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  • A kind of effervescent drug producing polylactic acid glycolic acid and its preparation method and application
  • A kind of effervescent drug producing polylactic acid glycolic acid and its preparation method and application
  • A kind of effervescent drug producing polylactic acid glycolic acid and its preparation method and application

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Experimental program
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Effect test

Embodiment 1

[0029] Weigh 1 g PLGA (molecular weight 10,000 Daltons, LA:GA=1:1, purchased from Jinan Daigang Biotechnology Co., Ltd.), mix it with 2 mL NMP, and stir at room temperature for 12 hours to obtain a clear and transparent solution. Take 0.1g of citric acid and 0.1g of sodium bicarbonate, mix them evenly with the above PLGA solution, and ultrasonically disperse (output power: 500W) at room temperature for 0.5 hours, so that citric acid and sodium bicarbonate are evenly dispersed in the above PLGA solution. Weigh 5mg of Dox (purchased from Beijing Huafeng Pharmaceutical Co., Ltd.), and ultrasonically disperse in the above PLGA / PT dispersion system (output power: 500W) at room temperature for 0.5 hours to obtain PLGA / PT / Dox. Take 50 μL of PLGA / PT / Dox solution and quickly pour it into water. After the solution completely changes phase, the PLGA / PT / Dox scaffold is obtained. The preparation methods of PLGA, PLGA / PT and PLGA / Dox scaffolds are the same as above.

[0030] From figure 1...

Embodiment 2

[0032] Take 0.5 mL of PLGA and PLGA / PT / Dox in Example 1, respectively, and inject them into cryovials filled with distilled water. After the phase transition is complete, place the frozen tube in a shaker at 37°C for incubation. At each predetermined time point, pipette 1 mL of DOX-containing distilled water and add 1 mL of the corresponding fresh buffer solution. The concentration of released DOX was determined by the standard curve, the cumulative total release of DOX at different time points was calculated, and the release of DOX by the PLGA / PT / Dox scaffold was analyzed. In order to study the effect of HIFU on the generation speed of air bubbles and drug release speed, PLGA and PLGA / PT / Dox scaffolds were respectively stimulated with HIFU (180W, stimulation time 400ms, interval 200ms, stimulation times 6 times) after incubation for 5min, and the bubbles were observed. and drug release, results such as figure 2 shown. Before and after HIFU stimulation, the PLGA scaffolds ...

Embodiment 3

[0034] Eighteen New Zealand white rabbits bearing VX2 tumors (tumor diameter about 1.5-2.0 cm) were randomly divided into 6 groups. Inject ①30 μL normal saline (blank control group); ②30 μL PLGA / Dox; ③30 μL PLGA, supplemented with HIFU stimulation; ④30 μL PLGA / PT, supplemented with HIFU stimulation; ⑤30 μL PLGA / Dox, supplemented with HIFU stimulation; PT / Dox, supplemented by HIFU stimulation (180W, stimulation time 400ms, interval 200ms, stimulation times 6 times). After treatment, the tumor volume of nude mice was recorded every other day. On the 14th day after treatment, blood was taken from the ear veins of each experimental rabbit in group ⑥, and the blood indicators were tested; on the 28th day after treatment, the experimental rabbits in group ⑥ were euthanized, and tissue sections were made for each major organ, and analyzed by H&E staining The pathological changes of each major organ (another consistent healthy rabbit was used as a control).

[0035] The experimental...

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Abstract

The invention discloses a bubble-producing polylactide acid-glycolic acid effervescence drug. The bubble-producing polylactide acid-glycolic acid effervescence drug comprises polylactide acid-glycolic acid, an effervescence substance, a chemotherapy drug and an organic solvent, wherein the concentration of polylactide acid-glycolic acid in the organic solvent is 0.1-1.0g / mL; the effervescence substance consists of organic acid and alkaline substance, the concentration of organic acid in the organic solvent is 0.1-0.5g / mL, and the concentration of alkaline substance in the organic solvent is 0.1-0.5g / mL; the concentration of chemotherapy drug in the organic solvent is 1-10g / mL. The invention also provides a preparation method of the bubble-producing polylactide acid-glycolic acid effervescence drug and a bubble-producing polylactide acid-glycolic acid effervescence drug stent material. The bubble-producing polylactide acid-glycolic acid effervescence drug has the advantages that under the irradiation action of HIFU (high intensity focused ultrasound), the effervescence substance produces air bubbles in the stent material, so that the ablation effect of HIFU on tumors is improved; the loaded chemotherapy drug is released out, and the capability of stent chemotherapy treating the tumors is realized.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and relates to a medicine for treating tumors, in particular to a polylactic-glycolic acid effervescent medicine for producing foam, a preparation method and application thereof. Background technique [0002] As we all know, cancer has become a huge killer that threatens human life and health in today's society. With the development of material science and nano-engineering, the development of tumor diagnosis and treatment methods with high curative effect and low toxicity is of great significance to improve the quality of human life and develop the national economy. High-intensity focused ultrasound (HIFU) treatment of tumors is a micro / non-invasive treatment method for tumors that has emerged in recent years. It uses the characteristics of good directionality and strong penetrating ability of ultrasound. Focuses on the tumor target and deposits acoustic energy into the tissue in a minimally i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K31/704A61P35/00
CPCA61K9/0007A61K31/704A61K47/34
Inventor 王世革李想安潇刘璐黄明贤
Owner UNIV OF SHANGHAI FOR SCI & TECH
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