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Paclitaxel lipid nanoparticle injection liquid with anti-tumor activity

A technology of lipid nanoparticles and anti-tumor activity, which is applied in anti-tumor drugs, liquid delivery, emulsion delivery, etc. It can solve the problem of drug resistance of tumor cells to chemotherapeutic drugs, limit SLN drug loading capacity, and multiple drug release curves Changes and other issues to achieve the effect of overcoming tumor drug resistance, excellent tumor drug resistance, and avoiding allergic reactions or toxic reactions

Inactive Publication Date: 2013-01-16
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] (3) Apoptosis resistance: Most anticancer drugs cause cell death through apoptosis, and the deletion of pro-apoptotic genes or overexpression of anti-apoptotic gene Bcl-2 will correspondingly lead to tumor cell resistance to chemotherapeutic drugs. drug resistance
[0015] The second strategy for reversing tumor multidrug resistance mostly uses chemotherapy sensitizers and drug resistance regulators targeting P-gp or other drug-resistant proteins: such as verapamil, cyclostimulin, etc., but the toxic doses of these drugs Similar to the effective dose, it is difficult to achieve an effective concentration that can be reversed, and there are still problems such as a single target and low selectivity
But because of this, the limited space between well-aligned crystals limits the drug-loading capacity of SLNs
In addition, SLN still has many potential problems: limited drug loading, variable drug release profile, drug leakage during storage, etc.
These problems greatly limit the use of SLN

Method used

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  • Paclitaxel lipid nanoparticle injection liquid with anti-tumor activity
  • Paclitaxel lipid nanoparticle injection liquid with anti-tumor activity
  • Paclitaxel lipid nanoparticle injection liquid with anti-tumor activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] The prescription and preparation technology of embodiment 1 paclitaxel preparation

[0064] Prescription 1:

[0065]Paclitaxel 1 %

[0066] Oleic acid 0.8%

[0067] Phospholipids 2 %

[0068] Vitamin E 5%

[0069] Cholesterol 1 %

[0070] DSPE-PEG2000 0.5%

[0071] Sucrose 10%

[0072] EDTA0.5%

[0073] The rest is water for injection.

[0074] Preparation method 1:

[0075] (1) Dissolve the prescribed amount of vitamin E, phospholipids, oleic acid, cholesterol, DSPE-PEG2000, and paclitaxel in an appropriate amount of absolute ethanol, and remove the ethanol by rotary evaporation under reduced pressure to obtain the lipid phase;

[0076] (2) Mix sucrose, EDTA, and water for injection, and stir magnetically until each part is dissolved to obtain the aqueous phase;

[0077] (3) The lipid phase was heated and stirred at 60°C, the water phase was added dropwise to the lipid phase, and stirred rapidly for 10 minutes to obtain milky white colostrum;

[0078] (4) Pl...

Embodiment 2

[0085] Prescription 2:

[0086] Paclitaxel 0.5%

[0087] Oleic acid 0.65%

[0088] Lecithin 2.6%

[0089] Vitamin E 6 %

[0090] DSPE-PEG2000 1%

[0091] Sucrose 10.4%

[0092] Sodium cholate 0.7%

[0093] EDTA0.1%

[0094] The rest is water for injection.

[0095] Preparation method 2:

[0096] (1) Dissolve the prescribed amount of vitamin E, lecithin, oleic acid, paclitaxel, and DSPE-PEG2000 in an appropriate amount of absolute ethanol, and remove the ethanol by rotary evaporation under reduced pressure to obtain the lipid phase;

[0097] (2) Mix sucrose, sodium cholate, and EDTA with water for injection, and stir magnetically until each part is dissolved to obtain an aqueous phase;

[0098] (3) The lipid phase was heated and stirred at 60°C, the water phase was added dropwise to the oil phase, and stirred rapidly for 10 minutes to obtain milky white colostrum;

[0099] (4) Place the colostrum in a high-pressure milk homogenizer, homogenize it with a pressure of 11...

Embodiment 3

[0101] Prescription 3:

[0102] Paclitaxel 3 %

[0103] Oleic Acid 2.4%

[0104] Lecithin 4 %

[0105] Vitamin E 15%

[0106] Cholesterol 1.2%

[0107] DSPE-PEG2000 1%

[0108] Sucrose 10.05%

[0109] Sodium cholate 0.7%

[0110] EDTA0.5%

[0111] The rest is water for injection.

[0112]

[0113] Preparation method 3:

[0114] (1) Dissolve the prescribed amount of vitamin E, lecithin, oleic acid, paclitaxel, cholesterol, and DSPE-PEG2000 in an appropriate amount of absolute ethanol, and remove the ethanol by rotary evaporation under reduced pressure to obtain the lipid phase;

[0115] (2) Mix sucrose, sodium cholate, and EDTA with water for injection, and stir magnetically until each part is dissolved to obtain an aqueous phase;

[0116] (3) The lipid phase was heated and stirred at 60°C, the water phase was added dropwise to the oil phase, and stirred rapidly for 10 minutes to obtain milky white colostrum;

[0117] (4) Place the colostrum in a high-pressure milk ...

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PUM

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Abstract

The invention provides paclitaxel lipid nanoparticle injection liquid, which comprises paclitaxel medicine, lipid materials, water for injection, surfactant, stabilizers and metal ion chelating agents. Most medicine is wrapped inside lipid, the direct contact between the medicine and blood or other liquid is avoided, and the local irritation of the medicine on the injection position is reduced, and the toxicity is reduced. No any organic solvents are contained, no solvents with toxicity and irritation on human bodies are contained, and no irritation and no sensitization are caused on the human bodies. The adverse reaction of the existing preparation caused by the recipe problem can be eliminated, and the goals of safety and efficiency are reached. Meanwhile, the paclitaxel lipid nanoparticle injection liquid has the excellent characteristic that the tumor medicine resistance is overcome, and the cure efficiency of the paclitaxel on the existing various tumors is greatly improved.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a paclitaxel lipid nanoparticle injection, in particular to a preparation method of a novel lipid nanoparticle preparation containing paclitaxel and vitamin E, which has high-efficiency antitumor activity and overcomes tumor drug resistance. Background technique [0002] Paclitaxel is a natural compound isolated from this slow-growing evergreen tree of the Taxus family. It has obvious and unique anti-tumor curative effect. Paclitaxel blocks mitosis by acting on intracellular tubulin, resulting in the death of rapidly dividing cancer cells. At the same time, paclitaxel can induce apoptosis, regulate immunity, and kill or inhibit tumor cells. The powerful and unique anti-tumor mechanism has made paclitaxel the most popular, best-selling, most scarce, most expensive, and also the most widely used anti-tumor drug in the world today. Paclitaxel is currently mainly applicable to ovarian cancer...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/14A61K31/337A61P35/00
Inventor 虞和永游剑李云龙胡富强袁弘杜永忠
Owner ZHEJIANG UNIV
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