Modified chitosan targeted medicament carrying nano microsphere and preparation method thereof

A drug-loaded nano- and nano-microsphere technology, which is applied in the direction of pharmaceutical formulations, antineoplastic drugs, drug combinations, etc., to achieve the effects of delayed release, high killing rate, and high drug encapsulation rate

Inactive Publication Date: 2010-06-02
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Aiming at the shortcomings of the existing chitosan-based nano-microspheres, the purpose of the present invention is to provide a nano-microsphere with small particle size, high drug encapsulation efficiency, large drug loading capacity, high coupling efficiency of targeted biomolecules, Preparation of Modified Chitosan Targeted Drug-loaded Nanospheres with Mild Conditions and Strong Targeting

Method used

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  • Modified chitosan targeted medicament carrying nano microsphere and preparation method thereof
  • Modified chitosan targeted medicament carrying nano microsphere and preparation method thereof
  • Modified chitosan targeted medicament carrying nano microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1: Preparation method and application of Tf-ADR / CMCS nanospheres

[0038](1) Preparation of carboxymethyl chitosan (CMCS): 5 g of chitosan (CS) was dissolved in 50 ml of isopropanol solution, and 20 ml of NaOH solution with a mass concentration of 50% was added under stirring conditions to make chitosan The sugar swelled under alkaline conditions, and was stored at 0 °C for 6 h to make it completely alkalized; at 30 °C, 2 g of solid chloroacetic acid was added to the above solution to prepare a crude product of CMCS; glacial acetic acid was used to adjust the pH of the solution to 7.0, Then wash with ethanol solution in turn, remove small molecular impurities by dialysis bag dialysis, and dry to obtain white powdery CMCS.

[0039] (2) Preparation of ADR / CMCS nano-microspheres: CMCS, carbodiimide (EDAC) and ADR were stirred and reacted for 10 min under the acetic acid buffer solution medium of pH 4.0 at a molar ratio of 1.0:0.5:0.2, and centrifuged. Collected an...

Embodiment 2

[0043] Example 2: Preparation method and application of Tf-ADR / CMCS nanospheres

[0044] (1) Preparation of carboxymethyl chitosan (CMCS): Dissolve 15 g of chitosan (CS) in 150 ml of isopropanol solution, add 100 ml of NaOH solution with a mass concentration of 50% under stirring conditions to make chitosan Swell under alkaline conditions, store at 10 °C for 18 hours to make it completely alkalized; at 50 °C, add 10 g of solid chloroacetic acid to the above solution to prepare a crude product of CMCS; use glacial acetic acid to adjust the pH of the solution to 7.0, then Wash with ethanol solution in turn, remove small molecular impurities by dialysis bag dialysis, and dry to obtain white powdery CMCS.

[0045] (2) Preparation of ADR / CMCS nano-microspheres: CMCS, carbodiimide (EDAC) and ADR were stirred and reacted for 40 min under the acetic acid buffer solution medium of pH 7.0 at a molar ratio of 5.0:1.5:0.8, and centrifuged. Collected and dried to prepare ADR / CMCS nanosphe...

Embodiment 3

[0049] Example 3: Preparation method and application of Tf-5-Fu / CMCS nanospheres

[0050] (1) Preparation of carboxymethyl chitosan (CMCS): Dissolve 6 g of chitosan (CS) in 60 ml of isopropanol solution, add 30 ml of NaOH solution with a mass concentration of 50% under stirring conditions, and let the chitosan The sugar swelled under alkaline conditions, and was stored at 2 °C for 7 hours to make it completely alkalized; at 35 °C, 6 g of solid chloroacetic acid was added to the above solution to prepare a crude product of CMCS; glacial acetic acid was used to adjust the pH of the solution to 7.0, Then wash with ethanol solution in turn, remove small molecular impurities by dialysis bag dialysis, and dry to obtain white powdery CMCS.

[0051] (2) Preparation of 5-Fu / CMCS nano-microspheres: CMCS, carbodiimide (EDAC) and 5-Fu were stirred at a molar ratio of 1.0:0.5:0.5 in an acetate buffer solution at pH 4.0. The reaction was carried out for 10 min, collected by centrifugation,...

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Abstract

The invention provides a modified chitosan targeted medicament carrying nano microsphere and a preparation method thereof. The method comprises the following steps of: modifying chitosan into carboxymethyl chitosan; then crosslinking an active amino group on a medicament molecule with an active carboxyl on the carboxymethyl chitosan by using a biological cross-linking agent and preparing a medicament carrying nano microsphere; and finally, connecting the targeted biological molecule to the surface of the medicament carrying microsphere by a chemical modification method and obtaining the modified chitosan targeted medicament carrying nano microsphere. The medicament carrying nano microsphere has small particle diameter, high medicament encapsulating rate, large medicament carrying quantity, high coupling efficiency of targeted biological molecules, mild preparation condition, strong targeted performance and low medicament toxic and side effect and can improve the targeted function and the slow release function on tumor cells, thereby strengthening the killing rate for the tumor cells.

Description

technical field [0001] The invention relates to the application of biological nanomaterials in the field of biomedicine, and discloses a modified chitosan targeting drug-loading nano-microsphere with the ability to actively target tumor cells and a preparation method thereof. Background technique [0002] The active targeting and low toxicity and side effects of anti-tumor drugs are very important for the clinical treatment of diseases. As a drug carrier, how to maximize the efficacy of the drug, reduce the frequency and dosage of medication, and improve the utilization rate and efficacy of the drug is a key issue. One of the very important questions. Studies have shown that an ideal anti-tumor drug-loading system can selectively accumulate anti-tumor drugs in cancerous sites in the body, reduce the toxic and side effects of drugs on normal tissues, improve drug bioavailability, and thus improve drug efficacy. This is the current anti-tumor drug. Hot spots in the field of r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/48A61K47/36A61K47/42A61K47/22A61K31/704A61K31/513A61P35/00A61K47/61A61K47/69
Inventor 杨培慧蔡怀鸿张文豪蔡继业
Owner JINAN UNIVERSITY
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