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Method for preparing folic acid coupled chitosan-hydrochloric acid mitoxantrone nano-particle

A technology of mitoxantrone hydrochloride and nano-particles is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, and pharmaceutical formulas, which can solve the problems of long preparation time, long reaction time, and easy coupling agent. Residue and other problems, to achieve the effect of improving controlled release and targeting, shortening the reaction time, and avoiding cytotoxicity

Inactive Publication Date: 2014-03-19
GUANGDONG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, the method for coupling folic acid molecules to drug carriers in the prior art has the disadvantages of long reaction time and cumbersome steps on the one hand, resulting in long preparation time and low production efficiency; on the other hand, the used coupling agent and The organic solvent used as the liquid phase is usually toxic, and the coupling agent is likely to remain, and the residual coupling reagent is likely to cause cytotoxicity to the body and inactivation of macromolecules

Method used

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  • Method for preparing folic acid coupled chitosan-hydrochloric acid mitoxantrone nano-particle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The preparation method of folic acid-coupled chitosan-mitoxantrone hydrochloride nanoparticles comprises the following steps:

[0037] Step 1, mixing the mitoxantrone hydrochloride solution with the chitosan acetic acid solution to obtain a mixed solution of chitosan and mitoxantrone hydrochloride;

[0038] Wherein, the mitoxantrone hydrochloride solution is prepared by dissolving mitoxantrone hydrochloride in water. In this embodiment, the mass / volume concentration of the mitoxantrone hydrochloride solution is 1 mg / mL.

[0039]Wherein, chitosan acetic acid solution is prepared by dissolving chitosan in acetic acid solution, in the present embodiment, the mass / volume concentration of chitosan acetic acid solution is 2mg / mL, and the mass percent concentration of acetic acid solution is 2%.

[0040] Step 2, under the condition of magnetic stirring and water bath heating, use a syringe to drip the mixture of chitosan and mitoxantrone hydrochloride into the ammonium fo...

Embodiment 2

[0050] The preparation method of folic acid-coupled chitosan-mitoxantrone hydrochloride nanoparticles comprises the following steps:

[0051] Step 1, mixing the mitoxantrone hydrochloride solution with the chitosan acetic acid solution to obtain a mixed solution of chitosan and mitoxantrone hydrochloride;

[0052] Wherein, the mitoxantrone hydrochloride solution is prepared by dissolving mitoxantrone hydrochloride in water. In this embodiment, the mass / volume concentration of the mitoxantrone hydrochloride solution is 3 mg / mL.

[0053] Wherein, chitosan acetic acid solution is prepared by dissolving chitosan in acetic acid solution, in the present embodiment, the mass / volume concentration of chitosan acetic acid solution is 5mg / mL, and the mass percentage concentration of acetic acid solution is 4%.

[0054] Step 2, under the condition of magnetic stirring and heating in a water bath, use a syringe to drip the mixture of chitosan and mitoxantrone hydrochloride into the ammoni...

Embodiment 3

[0064] The preparation method of folic acid-coupled chitosan-mitoxantrone hydrochloride nanoparticles comprises the following steps:

[0065] Step 1, mixing the mitoxantrone hydrochloride solution with the chitosan acetic acid solution to obtain a mixed solution of chitosan and mitoxantrone hydrochloride;

[0066] Wherein, the mitoxantrone hydrochloride solution is prepared by dissolving mitoxantrone hydrochloride in water. In this embodiment, the mass / volume concentration of the mitoxantrone hydrochloride solution is 0.5 mg / mL.

[0067] Wherein, chitosan acetic acid solution is prepared by dissolving chitosan in acetic acid solution, in the present embodiment, the mass / volume concentration of chitosan acetic acid solution is 1mg / mL, and the mass percentage concentration of acetic acid solution is 1%.

[0068] Step 2, under the condition of magnetic stirring and water bath heating, use a syringe to drip the mixture of chitosan and mitoxantrone hydrochloride into the ammonium ...

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Abstract

The invention relates to the technical field of tumor targeted medicaments, and in particular relates to a method for preparing a folic acid coupled chitosan-hydrochloric acid mitoxantrone nano-particle. The method comprises the following steps: 1, mixing a hydrochloric acid mitoxantrone solution with chitosan acetum so as to obtain a mixture solution of chitosan and hydrochloric acid mitoxantrone; 2, adding the mixture solution of chitosan and hydrochloric acid mitoxantrone into a folic acid amino solution, subsequently continuing adding a polysodium phosphate solution into the folic acid amino solution, and uniformly mixing so as to obtain a folic acid-chitosan-hydrochloric acid mitoxantrone microsphere water dispersed system; 3, centrifuging the acid-chitosan-hydrochloric acid mitoxantrone microsphere water dispersed system so as to obtain precipitate, washing the precipitate, and subsequently freezing to dry and obtain the folic acid coupled chitosan-hydrochloric acid mitoxantrone nano-particle. By adopting the method, application of an organic solvent is prevented, the reaction time is greatly shortened, and the prepared nano-particle has a remarkable targeting function on tumor cells, and is good in biocompatibility.

Description

technical field [0001] The invention relates to the technical field of anti-tumor targeted drugs, in particular to a preparation method of folic acid-coupled chitosan-mitoxantrone hydrochloride nanoparticles. Background technique [0002] Antineoplastic drugs often have the disadvantage of low selectivity. While killing tumor cells, they may also kill normal cells in the body. The toxic and side effects are relatively large, which brings great pain to patients. Folate receptor is a specific target for tumor selective drug delivery. The activity and quantity of folate receptor on the membrane surface of about 30% of tumor cells (such as ovarian cancer cells, colorectal cancer cells, lung cancer cells, kidney cancer cells, etc.) significantly higher than normal cells. In pharmacology, due to the specificity, selectivity, and strong affinity of the binding between the receptor and its ligand, the use of the ligand as a drug carrier or coupling with the carrier can increase the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/36A61K47/22A61K31/136A61P35/00
Inventor 王炜
Owner GUANGDONG MEDICAL UNIV
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