Shell layer dropping type nanometer medicine carrier preparation based on amphiphilic block copolymer and preparation method thereof

A nano-drug carrier and amphiphilic block technology, which is applied in the fields of polymer materials and medical engineering, can solve the problems of repeated administration, affect the curative effect, and low drug bioavailability, and achieve prolonging blood circulation time and improving biological Utilization, to achieve the effect of localized release

Inactive Publication Date: 2011-01-26
苏州同科生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Low-molecular and macromolecular drugs widely used at present have their own disadvantages: (1) Low-molecular drugs are administered orally or by injection, and the drug concentration in the body in a short period of time exceeds the actual demand, and lacks the selectivity of entering the human body; fast metabolism , the half-life is short, the concentration in the body will decrease quickly and affect the curative effect, so it needs to be given in large doses, and the high drug concentration will enhance the side effects of the drug
(2) Biomacromolecular drugs are easy to be inactivated by enzymolysis in the body, and the biological half-life is short, requiring repeated administration; also subject to restrictions such as the immune system, tissues, cell membranes, etc., most of the

Method used

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  • Shell layer dropping type nanometer medicine carrier preparation based on amphiphilic block copolymer and preparation method thereof
  • Shell layer dropping type nanometer medicine carrier preparation based on amphiphilic block copolymer and preparation method thereof
  • Shell layer dropping type nanometer medicine carrier preparation based on amphiphilic block copolymer and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Preparation of Nano-drug Carrier Preparation Based on Amphiphilic Copolymer

[0035] Weigh 50 mg of triblock copolymer of polyethylene glycol and polycaprolactone and 10 mg of paclitaxel, dissolve in 60 mL of tetrahydrofuran, and ultrasonicate for 10 min at room temperature to fully disperse and dissolve the polymer and drug to form a transparent organic phase; The obtained organic phase solution was placed in a dialysis bag, and then dialyzed in 1 L of water for 24 hours, and the dialysate was changed every 3 hours. After the dialysis, the aqueous solution of drug-loaded micelles formed in the dialysis bag was collected, and then freeze-dried for 20 hours to obtain a powdery solid preparation. The particle size distribution of the particles was measured with a dynamic laser light scattering instrument, and the polydispersity was 0.041. The TEM photos show that the average particle size of the nanoparticles is 92nm, the particles are spherical, and the disper...

Embodiment 2

[0036] Example 2 Preparation of Nano-Drug Carrier Preparation Based on Amphiphilic Copolymer

[0037] Weigh 30 mg of a two-block copolymer of polyethylene glycol and polyleucine and 8 mg of doxorubicin, dissolve it in a mixed solvent of 20 mL of N,N-dimethylformamide and 20 mL of tetrahydrofuran, and sonicate at room temperature for 10 min to polymerize Drugs and drugs are fully dispersed and dissolved to form a transparent organic phase; the prepared organic phase solution is placed in a dialysis bag, then dialyzed in 500 mL of water for 30 hours, and the dialysate is changed every 4 hours. After the dialysis, the aqueous solution of drug-loaded micelles formed in the dialysis bag was collected, and then freeze-dried for 24 hours to obtain a powdery solid preparation. The particle size distribution of the particles was measured with a dynamic laser light scattering instrument, and the polydispersity was 0.107. The TEM photos show that the average particle size of the nanopar...

Embodiment 3

[0038] Example 3 Preparation of Nano-Drug Carrier Preparation Based on Amphiphilic Copolymer

[0039] Weigh 80mg of a diblock copolymer of poly-N-isopropylacrylamide and polycaprolactone and 20mg of camptothecin, dissolve it in 100mL of N,N-dimethylformamide, and ultrasonicate for 15min at room temperature to make the polymer and The drug is fully dispersed and dissolved to form a transparent organic phase; the prepared organic phase solution is placed in a dialysis bag, and then dialyzed in 1.5L of water for 48 hours, and the dialysate is changed every 2.5 hours. After the dialysis, the aqueous solution of drug-loaded micelles formed in the dialysis bag was collected, and then freeze-dried for 18 hours to obtain a powdery solid preparation. The particle size distribution of the particles was measured with a dynamic laser light scattering instrument, and the polydispersity was 0.063. The TEM photos show that the average particle size of the nanoparticles is 84nm, the particle...

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Abstract

The invention discloses a shell layer dropping type nanometer medicine carrier preparation based on an amphiphilic block copolymer and a preparation method thereof. The preparation is prepared from the following components in parts by weight: 1 to 20 parts by weight of active ingredient medicines, 10 to 200 parts by weight of amphiphilic block copolymers and 20 to 500 parts by weight of organic solvents. The nanometer medicine micelle carrier preparation is in a core-shell structure, the core of which is a hydrophobic chain segment used for wrapping active ingredients and the shell of which is an amphiphilic block copolymer hydrophilic chain segment, and a hydrophilic segment and a hydrophobic segment in the amphiphilic block copolymer are connected through a disulphide bond S-S. The medicine carrier preparation can be preserved easily and has the advantages of high stability, high medicine cladding ratio, large medicine loading capacity, low toxicity and high medicine bioavailability.

Description

technical field [0001] The invention belongs to the fields of polymer materials and medical engineering, and in particular relates to a shell detachable nano drug carrier preparation based on an amphiphilic block copolymer and a preparation technology thereof. Background technique [0002] Cancer is a common disease that endangers human life and health. With the development of society and economy and the change of human living habits, the incidence and mortality of cancer are on the rise. Chemotherapy is the basic method of cancer treatment. Chemotherapy is of great significance to the treatment of cancer and the control of metastasis of cancer cells. However, chemotherapy also faces many unsolved problems. Low-molecular and macromolecular drugs widely used at present have their own disadvantages: (1) Low-molecular drugs are administered orally or by injection, and the drug concentration in the body in a short period of time exceeds the actual demand, and lacks the selectivi...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K47/32A61K47/34
Inventor 任天斌李建波李永勇贾梦虹
Owner 苏州同科生物科技有限公司
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