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Chitosan-carrying mitomycin nano targeting preparation and preparation method thereof

A technology of chitosan nanometer and mitomycin, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., and can solve problems such as limited use

Inactive Publication Date: 2010-07-21
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But the slow-release material can only be used as an implant, limiting its usefulness

Method used

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  • Chitosan-carrying mitomycin nano targeting preparation and preparation method thereof
  • Chitosan-carrying mitomycin nano targeting preparation and preparation method thereof
  • Chitosan-carrying mitomycin nano targeting preparation and preparation method thereof

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preparation example Construction

[0023] Preparation of nanoparticles:

[0024] Take 1 g of chitosan with a molecular weight of 70,000 and a degree of deacetylation of 95%, and dissolve it in 500 ml of acetic acid buffer solution with a pH of 5.1 to obtain a chitosan solution. Get 50ml of this chitosan solution, under vigorous stirring, slowly add 12.5ml, the sodium tripolyphosphate solution of 2mg / ml, obtain the chitosan nano particle solution of ion cross-linking; Take the prepared ion cross-linking chitosan Add 0.588, 5% glutaraldehyde aqueous solution to the nanoparticle solution, cross-link at 37°C for 12 hours, and then reduce with excess sodium borohydride to finally prepare particles with a particle size of 240nm.

[0025] The prepared nanoparticles were diluted to 8 mg / ml, and 5 mg / ml of folic acid solution dissolved in 1 / 15M phosphate buffer with a pH of 7.4 was added at a mass ratio of nanoparticles to folic acid of 10:1. Add 3 times the mass of folic acid in EDC and react for 1 h to obtain folic a...

Embodiment 1

[0031] Take 5mg of the prepared succinic acid-modified mitomycin, add it to 2ml, 10mg / ml unmodified chitosan nanoparticle solution, add 25mg of EDC, stir and react at room temperature for 30min, after the reaction, dialyze for 3h The unreacted mitomycin and other by-products were removed to obtain chitosan nanoparticles with a drug loading of 12.56%.

Embodiment 2

[0033] Get prepared succinic acid-modified mitomycin 5mg, join 2ml, 10mg / ml folic acid-modified chitosan nanoparticles (folic acid content 5%) solution, add 25mg of EDC, stir at room temperature for 30min, After the reaction was finished, unreacted mitomycin and other by-products were removed by dialysis for 3 hours to obtain chitosan nanoparticles with a drug loading capacity of 8.81%.

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Abstract

The invention discloses a chitosan-carrying mitomycin nano targeting preparation and a preparation method thereof, which relate to a medicine-carrying chitosan nano particle. The invention provides a chitosan-carrying mitomycin nano targeting preparation and a preparation method thereof. The chitosan-carrying mitomycin nano targeting preparation comprises chitosan nano particles for connecting mitomycin, which are dispersed in water. The mass ratio of mitomycin to nano particles is 1:(2-10), and the concentration of the nano particles in water is 1-20 mg / ml. The method comprises the following steps: preparing the chitosan nano particles; preparing folic acid modified nano particles; preparing PEG modified nano particles; preparing mitomycin ester succinate; and adding the mitomycin ester succinate and the chitosan nano particles into different modified nano particles, adding 1-[3-(Dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride, obtaining the mitomycin-carried nano particles after reaction, and dialyzing to remove the unreacted mitomycin and other byproducts, thereby obtaining the chitosan-carrying mitomycin nano targeting preparation.

Description

technical field [0001] The invention relates to a drug-loaded chitosan nano particle, in particular to a chitosan-loaded mitomycin nano-targeting preparation and a preparation method thereof. Background technique [0002] Youhua Song et al. ([1]. Youhua Song, Hiraku Onishi, Yoshiharu Machida, Tsuneji Nagai. Drug release and antitumor characteristics of N-succinyl-chitosan-mitomycin C as an implant. Journal of Controlled Release 42(1996) 93-100; [ 2]. N-succinyl-chitosan as a drug carrier: water-insoluble and water-soluble conjugates Kato Y, Onishi H, Machida Y.Biomaterials.25 (2004) 907-915) have studied in detail the use of mitomycin Linking to the chitosan molecule modified by succinic acid prepares a drug-loaded implant slow-release material, and the implant slow-release material can continuously release the drug within one week. And it has achieved good results in inhibiting S-180 tumors. But the slow-release material can only be used as an implant, which limits its us...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/407A61K9/14A61P35/00A61K47/36A61K47/34A61K47/22A61K47/54A61K47/60A61K47/61A61K47/69
Inventor 张其清胡权侯振清
Owner XIAMEN UNIV
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