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Method for preparing chitosan-polyasparagic acid-5efudix nano particle

A technology of polyaspartic acid and nanoparticles, applied in the field of nanomaterials, can solve problems such as inconvenience to patients, rapid metabolism in the body, and side effects

Inactive Publication Date: 2008-05-21
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are many disadvantages in the clinical use of 5-FU, such as oral administration is not easy to absorb, metabolism in the body is fast, half-life is short (only 5-10min), toxic and side effects are large, and large doses of long-term intravenous infusion are required to achieve effective effects in the body. Concentration and duration of action. In addition, the absorption of 5-FU is irregular. If the concentration in the body is too high, toxic and side effects will occur, which will bring great inconvenience and pain to patients.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1: Preparation of 55.6wt% mass ratio CS-PAsp-5FU nanoparticles

[0031] Preparation of Chitosan Pharmaceutical Aqueous Solution

[0032] In a 150ml volumetric flask, add 0.3g of chitosan with a molecular weight of 17.9kDa and a degree of deacetylation of 99%, 0.84g of 36% acetic acid aqueous solution, and 0.6g of 5-fluorouracil, and then add water to 150mL. Stir at room temperature for 48 hours, and filter to obtain a chitosan and 5-fluorouracil aqueous solution with a concentration of 2.0 mg / ml.

[0033] Preparation of Polyaspartic Acid Sodium Salt Solution

[0034] In a 150ml volumetric flask, add 0.3g of polyaspartic acid with a molecular weight of 10.0kDa, dissolve it in 50g of water for a period of time, adjust the pH value to 9.0 with 40% sodium hydroxide, add water to 150mL, and mix well to obtain a concentration of 2.0mg / ml polyaspartic acid sodium salt solution.

[0035] Preparation of CS-PAsp-5FU nanoparticles

[0036] Take 0.5 g of the above-m...

Embodiment 2

[0037] Embodiment 2: Preparation of 12.5wt% mass ratio CS-PAsp-5FU nanoparticles

[0038] The preparation of chitosan and 5-fluorouracil aqueous solution is the same as example 1.

[0039] The preparation of polyaspartic acid sodium salt solution is the same as Example 1.

[0040] The preparation of CS-PAsp-5FU nanoparticles is the same as in Example 1, except that the amount of the chitosan drug aqueous solution is 4.0 g. A water dispersion system of blue opalescent CS-PAsp-5FU nanoparticles was obtained, with an average particle diameter of 220.5nm, a drug loading capacity of 32.5%, and an embedding rate of 30.1%.

Embodiment 3

[0041] Embodiment 3: Preparation of low degree of deacetylation chitosan CS-PAsp-5FU nanoparticles

[0042] Preparation of chitosan and 5-fluorouracil aqueous solution

[0043] Same as Example 1, except that the degree of deacetylation of chitosan is 75%.

[0044] The preparation of polyaspartic acid sodium salt solution is the same as Example 1.

[0045] Preparation of CS-PAsp-5FU nanoparticles

[0046] In the same example 1, a blue-white opalescent CS-PAsp-5FU nanoparticle aqueous dispersion system was obtained, with an average particle diameter of 278.5nm, a drug loading capacity of 23.7%, and an embedding rate of 34.5%.

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Abstract

The invention relates to a preparation method of chitosan aspartate 5-fluorouracil-loaded nanoparticle. The invention makes use of the process to form the ionic compound of chitosan and aspartate to carry out the loading of 5-fluorouracil, so as to prepare the chitosan aspartate 5-fluorouracil-loaded nanoparticle water dispersion system by changing the molecular weight, molar ratio, reaction conditions and other factors of the raw materials under the mild reaction conditions, and the nanoparticle powder is obtained by freeze drying. The chitosan aspartate 5-fluorouracil-loaded water dispersion system of the invention is the nanoparticle with even dispersion and spherical shape. The product of the invention can be re-dispersed into the nanoparticle in water and has certain target and sustained-release performances. The invention has simple method and easy obtainment of raw materials; compared with the oral formulations on the market, the intestinal absorption efficiency and the bioavailability of the invention are significantly improved after oral administration, so the invention has better efficacy on malignant tumors.

Description

technical field [0001] The invention belongs to the technical field of nanometer materials, and in particular relates to a method for preparing chitosan-polyaspartic acid-5-fluorouracil nanoparticles by ion crosslinking reaction. Background technique [0002] Nanoparticles have many advantages in drug delivery, such as slow release of drugs, thereby prolonging the action time of drugs; achieving the purpose of targeted delivery of drugs; Or avoid adverse reactions; it can improve the stability of the drug, which is beneficial to storage; it is also possible to establish some new routes of administration, including local administration in vivo, mucosal absorption administration, and oral administration of polypeptides. At present, the carriers that can be used to prepare drug nanoparticles mainly include synthetic, biodegradable, high molecular polymers and natural macromolecular systems. Synthetic biodegradable polymers include: polyanhydrides, polycaprolactones, polylactic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/513A61K9/14A61K47/36A61K47/48A61P35/00A61K47/61
Inventor 杨武利郑永丽王春旭府寿宽董玲沈锡中
Owner FUDAN UNIV
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