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Chitin medicine carrier, prepn. method and application thereof

A technology of chitosan and drugs, applied in the field of drug carriers, can solve the problems of low drug encapsulation rate and drug content, large particle size, etc., and achieve the effect of inhibiting cancer cell growth, small particle size, and high encapsulation rate

Inactive Publication Date: 2007-01-31
沈鹤柏
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the particle size of chitosan drug-loaded microspheres reported in the literature is relatively large, the particle size ranges from a few microns to several hundred microns, and the drug encapsulation efficiency and drug content are relatively low.

Method used

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  • Chitin medicine carrier, prepn. method and application thereof
  • Chitin medicine carrier, prepn. method and application thereof

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0061] In this embodiment, the microemulsion method and the uniform design theory are used to wrap 5-fluorouracil with chitosan to obtain spherical particles with a particle size of about 70 ± 20 nm. The specific implementation methods are as follows:

[0062] Preparation process: use the uniform design method to draw up the data, and carry out the optimal design and analysis of the experiment according to the following steps

[0063] 1. Preparation of microemulsion: use 10~30mg of chitosan (different degrees of deacetylation) and acetic acid solution of fluorouracil as the water phase, mix it with 5ml of oil phase at 25~45°C and ultrasonic conditions, and dissolve it in 10~20ml Span 80 to prepare W / O microemulsion;

[0064] 2. Add 1~3ml of glutaraldehyde (crosslinking agent) to the prepared microemulsion and store it for 15min~150min;

[0065] 3. Use infrared, TEM and other testing instruments for particle characterization;

[0066] 4. Analyze the particles prepared by each...

Embodiment 2

[0068] In this embodiment, the microemulsion method and the uniform design theory are used to wrap 5-fluorouracil with chitosan to obtain spherical particles with a particle size of about 180 ± 20 nm. The specific implementation methods are as follows:

[0069] Preparation process: use the uniform design method to draw up the data, and carry out the optimal design and analysis of the experiment according to the following steps

[0070] 5. Preparation of microemulsion: use 10~30mg of chitosan (different degrees of deacetylation) and acetic acid solution of fluorouracil as the water phase, mix it with 15ml of oil phase under the condition of 45~60℃ and ultrasonic, and dissolve it in 10~20ml Tween 20 to prepare W / O microemulsion;

[0071] 6. Add 1~3ml polyethylene glycol (cross-linking agent) to the prepared microemulsion and store it for 15min~150min;

[0072] 7. Use infrared, TEM and other testing instruments for particle characterization;

[0073] 8. Analyze the particles pr...

Embodiment 3

[0075] Determination of drug encapsulation efficiency and drug content.

[0076] Dissolve the prepared chitosan microspheres in the phosphate buffer solution of PH=7.4, since 5-Fu dissolves under alkaline conditions, it will be released from the microspheres, detect its content with UV, and calculate the drug loading and encapsulation rate.

[0077] Calculation results: the drug encapsulation rate is at least 50%. The minimum drug content is 20%.

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Abstract

A chitosan nanopartile (50-200 nm in diameter) used as the carrier of medicine, especially the 5-flurouracil is prepared by microemulsion method. It can be used for researching biological nano-technique, target medicine, cytosis and cancer therapy.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to a drug carrier technology. Background technique [0002] Fluorouracil drugs represented by 5-fluorouracil (5-Fu) are currently the main drugs for the treatment of digestive tract, breast and head and neck tumors. Due to the low fat solubility of 5-Fu, difficulty in oral absorption, and short biological half-life, in order to achieve effective blood concentration in clinical practice, large doses, continuous administration or repeated administration routes are often adopted, so it has great side effects, such as bone marrow Inhibition, gastrointestinal reactions, leukocyte and thrombocytopenia, etc. An ideal 5-Fu nano drug delivery system should meet the following conditions: biodegradability; good stability, and will not leak out the drug wrapped in it before reaching the tumor tissue; targeting; Concentrated in the tumor tissue; with sustained release effect, the ...

Claims

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Application Information

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IPC IPC(8): A61K47/36
Inventor 沈鹤柏陈燕朱晨华
Owner 沈鹤柏
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