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Mithramycin nano-particle suspension and preparation method thereof

Inactive Publication Date: 2017-09-15
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the clinical use of shimmermycin in tumor therapy requires a high dose, and its systemic toxicity limits the therapeutic effect

Method used

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  • Mithramycin nano-particle suspension and preparation method thereof
  • Mithramycin nano-particle suspension and preparation method thereof
  • Mithramycin nano-particle suspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0108] Example 1: Preparation of a suspension of scintillation nanoparticles

[0109] The basic process of preparing scintilaginous nanoparticles by emulsification solvent evaporation method is shown in the appendix. figure 1 .

[0110] The implementation steps of this embodiment are as follows:

[0111] A. Preparation of diblock copolymer solution

[0112] The mPEG-PLGA diblock copolymer (PEG molecular weight 5000Da; PLGA molecular weight 15000Da; lactic acid and glycolic acid molar ratio: 50 / 50) sold by Jinan Daigang Bioengineering Co., Ltd. was dissolved in ethyl acetate solvent to obtain a concentration of 30 mg / mL diblock copolymer ethyl acetate solution;

[0113] B, the preparation of the organic phase of fucoidin

[0114] To the ethyl acetate solution of the diblock copolymer described above was added the diblock copolymer in the ratio 1:2.2 of the ethyl acetate solution in milliliters to the mithramycin in milligrams, marketed by Sigma-Aldrich under the trade nam...

Embodiment 2

[0123] Example 2: Preparation of a Pseudomycin Nanoparticle Suspension

[0124] The implementation steps of this embodiment are as follows:

[0125] A. Preparation of diblock copolymer solution

[0126] The PEG-PLLA diblock copolymer (PEG molecular weight 3000Da; PLLA molecular weight 15000Da) sold by Jinan Daigang Bioengineering Co., Ltd. was dissolved in dichloromethane solvent to obtain a diblock copolymer dichloromethane with a concentration of 40 mg / mL. solution;

[0127] B, the preparation of the organic phase of fucoidin

[0128] In accordance with the ratio of dichloromethane solution in milliliters to 1:1.0 in milligrams of scintilbomycin SK, the scintilbomycin SK reported by the document JAmChem Soc. 2003 May 14; 125(19): 5745-53 was added to the above Diblock copolymer in dichloromethane solution, shake and dissolve, obtain a kind of organic phase that contains brightmycin SK;

[0129] C. Preparation of emulsifier solution

[0130] The emulsifier PVA is dissolv...

Embodiment 3

[0137] Example 3: Preparation of a Pseudomycin Nanoparticle Suspension

[0138] The implementation steps of this embodiment are as follows:

[0139] A. Preparation of diblock copolymer solution

[0140] The PEG-PDLA diblock copolymer (PEG molecular weight 5000Da; PDLA molecular weight 20000Da) sold by Jinan Daigang Bioengineering Co., Ltd. was dissolved in chloroform solvent to obtain a diblock copolymer chloroform with a concentration of 34mg / mL. solution;

[0141] B, the preparation of the organic phase of fucoidin

[0142] According to the ratio 1:1.6 of chloroform solution in milliliters to the Spotomycin SDK in mg, the Spotsomycin SDK reported by the document JAmChem Soc. 2003 May 14; 125(19): 5745-53 was added to the above-mentioned dimeric In the chloroform solution of the segmented copolymer, vibrating and dissolving to obtain an organic phase containing the Spotomycin SDK;

[0143] C. Preparation of emulsifier solution

[0144] Dissolving the emulsifier sodium ch...

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Abstract

The invention relates to a mithramycin nano-particle suspension and a preparation method thereof. The preparation method comprises the following steps: preparation of a diblock copolymer solution; preparation of an organic phase of mithramycin; preparation of an emulsifier solution; mixing and aftertreatment; etc. A mithramycin nano-particle prepared in the invention can retain the pharmacological activity of mithramycin; materials used in the invention are biocompatible materials, so the mithramycin nano-particle has the characteristic of application security and has good application prospect; meanwhile, the mithramycin nano-particle can be effectively enriched in the part of a transplanted tumor of a naked mouse and presents substantial treatment effect on transplanted tumors of human pancreatic cancer cells BxPC-3 in naked mice.

Description

【Technical field】 [0001] The invention belongs to the technical field of drug delivery. More specifically, the present invention relates to a kind of incandescent nanoparticle suspension, and also relates to a preparation method of the incandescent nanoparticle suspension. 【Background technique】 [0002] MithramycinA (MIT), also known as prukamycin, is a naturally occurring polyketide antitumor antibiotic belonging to the chloramylic acid family. Since it was approved for clinical application, it has been used as a chemotherapeutic drug to treat malignant tumors such as testicular embryonic carcinoma and glioma. Glaxinomycin can bind to the minor groove of the GC-rich region on DNA, and the main mechanism of action is to competitively inhibit the binding of transcription factor Sp1 to gene regulatory elements, thereby affecting the formation of DNA-protein complexes and regulating related genes. expression. Sp1 is a transcription factor with a zinc finger structure, which...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/34A61K31/704A61P35/00
CPCA61K9/1075A61K31/704A61K47/34
Inventor 刘旭杰李良甄永苏刘秀均赵春燕王瑞琪
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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