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Drug sustained-release system for treating tumours and preparation method thereof

A technology for drugs and tumors, which is applied to the drug sustained-release system for treating tumors and its preparation field, can solve the problems of drug waste and large dosage, and achieve the effects of reduced usage, high drug loading, and stable drug release.

Active Publication Date: 2011-11-02
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] When using dichloroacetate for anti-cancer, it has the advantages of simple, cheap and effective administration, and only acts on cancer cells without damaging normal cells. However, dichloroacetate is generally administered orally or intravenously. The dosage is relatively large, and the current curative effect range is generally 25mg / kg / day. Large doses of oral or intravenous dichloroacetate lead to infiltration of dichloroacetate in the whole body of patients, which not only causes waste of drugs, but also causes long-term use of large doses of dichloroacetate. Chloroacetate may cause liver cancer (Bull, R.J., Sanchez, I.M., Nelson, M.A., Larson, J.L., and Lansing, A.J. (1990). Toxicology 63, 341-359), and short-term administration of large doses of dichloroacetate Salt can also produce side effects such as sedation and nervous tremors

Method used

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  • Drug sustained-release system for treating tumours and preparation method thereof
  • Drug sustained-release system for treating tumours and preparation method thereof
  • Drug sustained-release system for treating tumours and preparation method thereof

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preparation example Construction

[0052] The present invention also provides a preparation method of a drug sustained-release system for treating tumors, comprising the following steps:

[0053] a) dissolving the biodegradable polymer, dichloroacetate and surfactant in a solvent to obtain a drug solution or drug emulsion, wherein the dichloroacetate accounts for the biodegradable polymer, The mass percent of the total mass of dichloroacetate and surfactant is 15% to 70%, and the mass percent of the total mass of said surfactant accounts for the biodegradable polymer, dichloroacetate and surfactant 0% to 15%;

[0054] b) Electrospinning the drug solution or drug emulsion obtained in step a) to obtain a drug sustained-release system for treating tumors.

[0055] In the present invention, the degradable polymer, dichloroacetate and surfactant are dissolved in a solvent to obtain a drug solution or a drug emulsion. Specifically, the drug solution is obtained when mixing according to the following steps:

[0056]...

Embodiment 1

[0087] 2.035g of polylactic acid (containing 2% D-configuration polylactic acid) with a viscosity-average molecular weight of 123,000 was dissolved in a mixed solvent to obtain a polymer solution, and the mixed solvent included 12mL chloroform and 3mL acetone; Add 0.359g of sodium dichloroacetate and 1mL of methanol into the drug solution, stir and dissolve to obtain a drug solution, the viscosity of the drug solution is 4.6cPa; the drug solution is added to a 10mL syringe for electrospinning, and the The parameters during electrospinning are as follows: the voltage is 40kV; the current is 0.2mA; the distance between the two poles is 15cm; the flow rate of the polymer solution at the spinneret is 0.08mL / min; Lactic acid fiber, wherein the mass percentage of sodium dichloroacetate is 15%.

[0088] The described polylactic acid fiber containing medicine is carried out scanning electron microscope and energy dispersive X-ray spectrometry (EDS) analysis, the result sees figure 2...

Embodiment 2

[0095] Seventy male and female KM mice were each subcutaneously inoculated with 0.1 mL of sarcoma S180 cells containing more than 1,000,000 living cells in the right abdomen, and 54 tumors with a particle size of 7.5 mm and a tumor volume of about 200mm 3 The mice were randomly divided into groups A, B and C3, with 18 mice in each group.

[0096] The polylactic acid fibers prepared in Comparative Example 1 and the drug-containing polylactic acid fibers prepared in Example 1 were respectively made into fiber mats, which were respectively covered on the mouse tumors by sticking, that is, group A was the free growth control group, Group B is the fiber mat control group prepared in Comparative Example 1, and Group C is the fiber mat treatment group prepared in Example 1.

[0097] On the 7th day, the 14th day and the 20th day of medication, 6 mice in each group were sacrificed, and the tumor residue was observed. The results are shown in Table 2. Table 2 shows the therapeutic effe...

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Abstract

The invention provides a drug sustained-release system for treating tumours, which comprises a drug carrier, a drug and a surface active agent. The drug carrier is a biodegradable polymer fibre. The drug is a dichloroacetic acid salt covered and loaded on the drug carrier. The surface active agent is covered and loaded on the drug carrier, wherein the drug accounts for 15-70 wt % of the drug sustained-release system and the surface active agent accounts for 0-15 wt % of the drug sustained-release system. The invention further provides a preparation method of the drug sustained-release system for treating the tumours. The drug sustained-release system can realize the sustained release of the local drug so that the concentration of the local drug around the tumours is in a scope of a therapeutic effect window; however, the drug concentration except the tumours and in body fluid is in a health scope, therefore, the utilization rate of the drugs is increased and the therapeutic effect is guaranteed as well as the usage amount of the drugs is reduced and the toxic side effects caused by large dosage of the drugs are reduced.

Description

technical field [0001] The invention belongs to the technical field of drug controlled release, in particular to a drug sustained release system for treating tumors and a preparation method thereof. Background technique [0002] Cancer is the number one killer of human health, but for a long time, human beings have not fully understood the pathogenic mechanism of cancer and effective methods for treating cancer. In 1930, Warburg (Warburg, O. (1930). Ueber den stoffwechsel der tumoren (London: Constable)) proposed the Warburg effect, that is, the respiration of cancer cells changed from aerobic respiration to aerobic respiration due to mitochondrial dysfunction. Glycolysis is dominant and a large amount of lactic acid is secreted. The metabolic model of aerobic glycolysis proposed by Warburg provides a new targeting point and apoptosis-inducing strategy for cancer therapy, that is, mitochondria can be used as a target for cancer therapy. [0003] Dichloroacetate (DCA), an i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/34A61P35/00
Inventor 黄宇彬刘大兴景遐斌陈学思
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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