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Folic acid-vincristine targeted and slow-released nano-microspheres, prepared method and application thereof

A technology of vincristine and nano-microspheres is applied in the directions of pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, which can solve the problems of low output, poor stability, high cost, etc. Regular round, smooth surface, uniform size effect

Inactive Publication Date: 2011-01-12
何彦津 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the stability of the combination of drugs and bioactive molecules such as antibodies is poor, and the molecular size, surface charge and properties of receptor binding sites of the two are changed after the combination, which may reduce the efficacy and targeting
In addition, the preparation process of McAb is complicated, the output is low, and the cost of relying on antibody-targeted therapy is high

Method used

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  • Folic acid-vincristine targeted and slow-released nano-microspheres, prepared method and application thereof
  • Folic acid-vincristine targeted and slow-released nano-microspheres, prepared method and application thereof
  • Folic acid-vincristine targeted and slow-released nano-microspheres, prepared method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Folic acid-vincristine targeted sustained-release nano-microspheres are made by the following method:

[0041] (1) 100 mg of polylactic acid-glycolic acid was dissolved in 5 ml of dichloromethane and acetone with a volume ratio of 4:1, and the oil phase was prepared for subsequent use;

[0042] (2) make solvent with deionized water, be mixed with the vincristine aqueous solution that mass concentration is 3%;

[0043] (3) Dissolve 10 mg of polyethylene glycol 4000 and hydroxyethyl cellulose in a mass ratio of 1:3 as an emulsifier in 2.5 ml of the vincristine aqueous solution, and stir in the dark until the emulsifier is completely dissolved to prepare The inner water phase is reserved;

[0044] (4) Add the inner water phase prepared in the step (3) dropwise to the oil phase prepared in the step (1) of 5 ml at 80 watts and ultrasonic dispersion for 2 minutes to form water / oil colostrum solution;

[0045] (5) under the ultrasonic dispersion condition of 120 watts, 3 mi...

Embodiment 2

[0053] Folic acid-vincristine targeted sustained-release nano-microspheres, made by the following method:

[0054] (1) Dissolving 100 mg of polylactic acid-glycolic acid in 4 ml of dichloromethane and acetone with a volume ratio of 5:1, made an oil phase for subsequent use;

[0055] (2) make solvent with deionized water, be mixed with the vincristine aqueous solution that mass concentration is 2%;

[0056] (3) Dissolve 10 mg of polyethylene glycol 4000 and hydroxyethyl cellulose in a mass ratio of 1:4 as an emulsifier in 2.5 ml of the vincristine aqueous solution, and stir in the dark until the emulsifier is completely dissolved to prepare The inner water phase is reserved;

[0057] (4) Add the inner water phase prepared in the step (3) dropwise to the oil phase prepared in the step (1) of 5 ml at 70 watts and ultrasonic dispersion for 3 minutes to form water / oil colostrum solution;

[0058] (5) under the ultrasonic dispersion condition of 110 watts, 4 minutes, the aqueous ...

Embodiment 3

[0062] Folic acid-vincristine targeted sustained-release nano-microspheres, made by the following method:

[0063] (1) 100 mg of polylactic acid-glycolic acid was dissolved in 6 ml of dichloromethane and acetone with a volume ratio of 3:1, and the oil phase was prepared for subsequent use;

[0064] (2) make solvent with deionized water, be mixed with the vincristine aqueous solution that mass concentration is 3%;

[0065] (3) Dissolve 10 mg of polyethylene glycol 4000 and hydroxyethyl cellulose in a mass ratio of 1:2 as an emulsifier in 2.5 ml of the vincristine aqueous solution, and stir in the dark until the emulsifier is completely dissolved to prepare The inner water phase is reserved;

[0066] (4) Add the inner water phase prepared in the step (3) dropwise to the oil phase prepared in the step (1) of 5 ml at 90 watts and ultrasonic dispersion for 1 minute to form water / oil colostrum solution;

[0067] (5) under the ultrasonic dispersion condition of 130 watts, 2 minute...

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Abstract

The invention discloses folic acid-vincristine targeted and slow-released nano-microspheres, a prepared method and an application thereof. The preparation method comprises the steps of: dissolving the polylactic acid-glycollic acid in the dichloromethane and acetone to form the oil phase; dissolving the polyethylene glycol and the hydroxyethylcellulose in the water solution of vincristine and stirring to form the inner water phase, and adding the inner water phase into the oil phase dropwise to form the water / oil initial emulsion solution; adding the water solution of O-carboxymethyl chitosan octadecyl hyamine containing the hydroxyethylcellulose and the connected folic acid into the initial emulsion solution to form the water / oil / water composite system; stirring and volatilizing the organic solvent to obtain the solidified microspheres; centrifuging the solidified microspheres, removing the separated large-sized microspheres, centrifuging again to obtain the separated solid microspheres, washing and dirying to obtain the discloses folic acid-vincristine targeted and slow-released nano-microspheres. The discloses folic acid-vincristine targeted and slow-released nano-microspheres of the invention have good effect, high local drug concentration, long action time and less adverse reaction.

Description

technical field [0001] The invention relates to a targeted slow-release nano-microsphere, a preparation method and use thereof. Background technique [0002] Orbital adenoid cystic carcinoma (ACC) is the most common malignant epithelial tumor of the lacrimal gland, and its high degree of malignancy and poor prognosis have been recognized [1] . The traditional treatment method is orbital enucleation, but the postoperative recurrence rate is still high. In recent years, comprehensive treatment methods including radiotherapy and chemotherapy have been gradually applied to ACC, which has reduced the recurrence rate to a certain extent, but the 10-year survival rate of patients is only 20%. This cancer often occurs in young people and severely impairs the workforce. At the same time, the disfigurement caused by orbital enucleation and many complications caused by radiotherapy and chemotherapy not only make it difficult for patients to adhere to treatment, but also seriously re...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/475A61K47/34A61K47/22A61P35/00A61P27/02A61K47/10A61K47/36A61K47/38
Inventor 何彦津常津林婷婷罗浩朱利民梁晓飞陈陆霞
Owner 何彦津
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