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Self-assembled nanoparticles for targeting delivery of paclitaxel and its preparation method and uses

A self-assembled nanoparticle and paclitaxel technology, which is applied in powder delivery, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., can solve problems such as unsuitable nanoparticles

Inactive Publication Date: 2014-05-07
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, TPGS is not suitable for the preparation of nanoparticles alone. Generally, it forms mixed micelles with other amphiphilic molecules, such as phospholipids, to improve its stability.

Method used

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  • Self-assembled nanoparticles for targeting delivery of paclitaxel and its preparation method and uses
  • Self-assembled nanoparticles for targeting delivery of paclitaxel and its preparation method and uses
  • Self-assembled nanoparticles for targeting delivery of paclitaxel and its preparation method and uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1: Optimization of the preparation process of paclitaxel self-assembled nanoparticles --- the influence of hydration temperature

[0041] Precisely weigh the prescribed amount of TPGS (40mg), Tween80 (20mg), MCT (25mg) and PTX (1mg), that is, TPGS:Tween80:MCT:PTX=40:20:25:1 (w:w:w:w ), ultrasonically dissolved in 2mL absolute ethanol, added to a 25mL round-bottomed flask, and the organic solvent was removed by rotary evaporation under reduced pressure to form a transparent film on the bottle wall, and then 1mL preheated distilled water was added, respectively Shake and hydrate at 25°C, 37°C and 50°C to obtain paclitaxel self-assembled nanoparticles (PSN). Table 1 shows the effects of different hydration temperatures on the particle size, distribution and encapsulation efficiency of self-assembled nanoparticles.

[0042] Table 1 Particle size, particle size distribution and encapsulation efficiency of paclitaxel self-assembled nanoparticles prepared at different...

Embodiment 2

[0046] Example 2: Paclitaxel Self-Assembled Nanoparticles Preparation Process Optimization------Influence of Unit Prescription Paclitaxel Dosage

[0047] Except for the following differences, paclitaxel self-assembled nanoparticles were prepared according to the method described in Example 1: the hydration temperature was set at 37°C, the dosage of TPGS (40mg), Tween80 (20mg), and MCT (25mg) in the prescription was fixed, and three The dosage of paclitaxel at different levels: 0.5mg, 1mg and 2mg, to investigate the influence of the dosage of paclitaxel in the unit prescription on the preparation process. Taking the particle size, its distribution and encapsulation rate as the indicators, the following table 2 shows the particle size, particle size distribution and encapsulation rate of paclitaxel self-assembled nanoparticles prepared with different dosages of paclitaxel.

[0048] Table 2

[0049]

[0050] * The nanoparticles prepared under this condition had poor stabilit...

Embodiment 3

[0052] Embodiment 3: Paclitaxel self-assembled nanoparticle preparation process optimization------MCT and the influence of emulsifier mass ratio

[0053] Except for the following differences, paclitaxel self-assembled nanoparticles were prepared according to the method described in Example 1: the amount of emulsifier in the fixed prescription (ie, TPGS40mg, Tween8020mg), the unit dosage was 1mg paclitaxel, and the hydration temperature was 37°C. Two levels of MCT (10mg, 25mg and 40mg) were investigated, that is, the mass ratios of MCT and emulsifiers (TPGS, Tween80) were 10 / 60, 25 / 60 and 40 / 60, respectively, to investigate the relationship between MCT and emulsification in the prescription The effect of the proportion of the agent on the preparation process. The particle size, distribution and encapsulation efficiency of the paclitaxel self-assembled nanoparticles prepared with different MCT ratios are shown in Table 3 below.

[0054] table 3

[0055]

[0056] * The nano...

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Abstract

The invention relates to self-assembled nanoparticles for targeting delivery of paclitaxel and its preparation method and uses, the self-assembled nanoparticles of the paclitaxel comprise by weight: 1000 parts of polyethylene glycol, 40 parts of vitamin E succinate, 20 parts of TWEEN80, 10-40 parts of medium chain triglycerides and 0.5-2 parts of the paclitaxel, the particle size of the self-assembled nanoparticles of the paclitaxel is 1-100nm, at the cellular level, the self-assembled nanoparticles of the paclitaxel can deliver the paclitaxel to drug-resistant cells, and can increase the chemotherapy sensitivity of the drug-resistant cells, and in the animal level, the self-assembled nanoparticles of the paclitaxel can targetedly deliver the paclitaxel to tumor sites, and can increase the inhibiting effect of chemotherapy drugs on drug-resistant tumor. By the design of the carrier, the sensibility of breast cancer and lung cancer drug resistant cells on the paclitaxel can be improved.

Description

technical field [0001] The invention belongs to the field of biotechnology, and in particular relates to a self-assembled nanoparticle used for targeted delivery of paclitaxel, its preparation method and application. Background technique [0002] Chemotherapy is an important method of comprehensive tumor treatment. It is a method of bringing drugs to tumor tissue through blood vessels for tumor treatment. It is sometimes called "cytotoxic therapy" because chemotherapy drugs are toxic to a certain extent. Cells in the body are more or less less will be damaged. Clinically, tumors of the same pathological type and stage are treated with the same chemotherapy regimen, but the curative effect is different. Some tumors are insensitive to further chemotherapy after remission and shrinkage after chemotherapy, which is mainly caused by the resistance of cancer cells to chemotherapy drugs, which is often one of the main reasons for chemotherapy failure. Drug resistance, also known ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/337A61K47/34A61K47/26A61K47/14A61P35/00
Inventor 李亚平卜辉辉张志文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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