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Recombination thermosensitivity vesica for gemcitabine hydrochloride high efficiency thermochemotherapyand preparation method thereof

A technology of gemcitabine hydrochloride and thermal chemotherapy, which is applied in the fields of polymer materials and biomedical engineering, can solve problems such as unrelated research, and achieve the effects of improving the quality of life, improving clinical efficacy, and enhancing cytotoxicity

Active Publication Date: 2018-10-12
JIANGSU QINGJIANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to effectively enhance the clinical efficacy of gemcitabine hydrochloride, the involved nano-drug carriers need to be designed according to the heat-sensitizing properties of the drug, but there is no relevant research at present

Method used

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  • Recombination thermosensitivity vesica for gemcitabine hydrochloride high efficiency thermochemotherapyand preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Weigh 20 mg of PLA- b -p(NIPAM- co -DMAM), wherein the molecular weight of PLA: p(NIPAM- co The molecular weight of -DMAM) is 3: 1, takes by weighing 40mg in addition, and particle diameter is the superparamagnetic nanoparticle MnFe of 8nm 2 o 4 , both were dissolved in 5ml of dichloromethane to obtain an organic phase.

[0027] Weigh 0.5 mg of gemcitabine hydrochloride and disperse in 1 ml of deionized water to obtain an aqueous phase.

[0028] Dissolve PVA with a molecular weight of 31000 in deionized water to prepare an aqueous solution with a concentration of 0.1 mg / mL.

[0029]Under the conditions of ice-water bath and ultrasonic, the water phase was dropped into the organic phase, and the primary emulsion was obtained after thorough mixing. Add 20mL of PVA aqueous solution to the primary emulsion in an ice-water bath and ultrasonic conditions to obtain a secondary emulsion. The secondary emulsion was dropped into 80 mL of deionized water under the conditio...

Embodiment 2

[0033] Weigh 40 mg of PCL- b -p(NIPAM- co -DMAM), wherein the molecular weight of PCL: p(NIPAM- co The molecular weight of -DMAM) is 5: 1, takes by weighing 60mg in addition, and particle diameter is the superparamagnetic nanoparticle Mn of 12nm 0.6 Zn 0.4 Fe 2 o 4 , both were dissolved in 8ml of dichloromethane to obtain an organic phase.

[0034] Weigh 2 mg of gemcitabine hydrochloride and disperse in 2 ml of deionized water to obtain an aqueous phase.

[0035] Dissolve PVA with a molecular weight of 47000 in deionized water to prepare an aqueous solution with a concentration of 0.05 mg / mL.

[0036] Under the conditions of ice-water bath and ultrasonic, the water phase was dropped into the organic phase, and the primary emulsion was obtained after thorough mixing. The primary emulsion was added with 60 mL of PVA aqueous solution under the conditions of ice-water bath and ultrasonic to obtain the secondary emulsion. The secondary emulsion was dropped into 200 mL of ...

Embodiment 3

[0040] Weigh 20 mg of PLGA- b -p(NIPAM- co -DMAM), wherein the molecular weight of PLGA: p(NIPAM- co The molecular weight of -DMAM) is 8: 1, takes by weighing 40mg in addition, and particle diameter is the superparamagnetic nanoparticle Mn of 16nm 0.4 Zn 0.6 Fe 2 o 4 , both were dissolved in 4ml of dichloromethane to obtain an organic phase.

[0041] Weigh 0.5 mg of gemcitabine hydrochloride and disperse in 0.8 ml of deionized water to obtain an aqueous phase.

[0042] Dissolve PVA with a molecular weight of 47,000 in deionized water to prepare an aqueous solution with a concentration of 0.1 mg / mL.

[0043] Under the conditions of ice-water bath and ultrasonic, the water phase was dropped into the organic phase, and the primary emulsion was obtained after thorough mixing. Add 40 mL of PVA aqueous solution to the primary emulsion in an ice-water bath under ultrasonic conditions to obtain a secondary emulsion. The secondary emulsion was dropped into 180 mL of deionized...

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Abstract

The invention discloses a recombination thermosensitivity vesica carrier for significantly improving the curative effect of gemcitabine hydrochloride high efficiency thermochemotherapy and a preparation method thereof, and belongs to the field of high molecular materials and medical engineering. The recombination thermosensitivity vesica is formed by a amphiphilic thermosensitivity polymer wrapping dewatering superparamagnetic nanoparticles and hydrophil gemcitabine hydrochloride by a double emulsion method; the medical gemcitabine hydrochloride is wrapped by a hydrophil core of the thermosensitivity vesica; and the dewatering superparamagnetic nanoparticles is wrapped by a double-layer dewatering film of the recombination thermosensitivity vesica. The recombination thermosensitivity vesica can accurately controls releasing of mediated magnetic hyperthermia and temperature-controlled drugs, so that interval action of chemotherapy and the thermochemotherapy of the gemcitabine hydrochloride is achieved, and the efficacy of the chemotherapy and the thermochemotherapy of the gemcitabine hydrochloride is maximized.

Description

technical field [0001] The invention belongs to the field of macromolecular materials and biomedical engineering, and specifically relates to a nano-carrier that can effectively improve the cytotoxicity of chemotherapy drug gemcitabine hydrochloride, thereby realizing high-efficiency thermal chemotherapy of gemcitabine hydrochloride. Background technique [0002] Gemcitabine hydrochloride is a typical cell cycle inhibitory drug, which usually acts on cells in the S phase, that is, cells in the rapid proliferation phase. Therefore, gemcitabine hydrochloride is mostly used in the treatment of highly malignant advanced or metastatic solid tumors, including non-small cell lung cancer, pancreatic cancer, bladder cancer, breast cancer and ovarian cancer, etc., and has broad market prospects. However, the metabolism of gemcitabine hydrochloride is very fast in the body, and the half-life is only 17 minutes. Therefore, in clinical application, a higher dosage must be ensured to main...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K9/127A61K47/34A61P35/00A61K31/7068
CPCA61K9/1273A61K31/7068A61K41/0052A61K47/34A61P35/00A61K2300/00
Inventor 屈阳辛渊蓉赖文龙王维许颖刘宏飞
Owner JIANGSU QINGJIANG PHARMA
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