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Elastic nano vesicle preparations containing paclitaxel or docetaxel and preparation thereof

A technology of docetaxel and nanovesicles, applied in the field of medicine, can solve problems such as death

Inactive Publication Date: 2008-07-02
TECHNICAL INST OF PHYSICS & CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when Tween 80 is used for intravenous injection, it can cause allergic reactions, including shock, dyspnea, hypotension, angioedema, urticaria and other allergic-like reaction symptoms
Some of these adverse reactions were very serious in clinical studies, and even death was reported.

Method used

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  • Elastic nano vesicle preparations containing paclitaxel or docetaxel and preparation thereof
  • Elastic nano vesicle preparations containing paclitaxel or docetaxel and preparation thereof
  • Elastic nano vesicle preparations containing paclitaxel or docetaxel and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～6

[0031] Soybean lecithin, paclitaxel, and 0.1% vitamin E were dissolved in an appropriate amount of ethanol, and after mixing evenly, the ethanol was volatilized by nitrogen gas, and then a certain amount of 5mM phosphate buffer solution containing sodium cholate was added to pH 6.5, and isopropanol was added to make the iso Propanol accounts for 10% of the total volume, stirred at room temperature for 1 hour, and then ultrasonicated in a water bath for 30 minutes to obtain a preparation containing elastic nanovesicles, wherein the elastic nanovesicles are suspended in the remaining components after the above components are mixed to form vesicles in the mixed solution. Wherein, the content of soybean lecithin and sodium cholate is as follows, the content of paclitaxel is 0.2%, and the content of isopropanol is 10%.

[0032] The free drug and vesicles were separated by Sephadex G-50 gel, the encapsulation efficiency was detected by HPLC, and the particle size was measured by las...

Embodiment 7～8

[0038]Soybean lecithin (phosphatidylcholine > 92%), docetaxel, ascorbyl palmitate and vitamin E are dissolved with an appropriate amount of ethanol, after mixing evenly, the ethanol is volatilized by rotary evaporation, and then a certain amount of aqueous solution containing sodium cholate is added, Add ethanol, stir at room temperature for 1 hour, and then ultrasonicate in a water bath for 30 minutes to obtain a preparation containing elastic nanovesicles, which is suspended in a mixed solution of various components remaining after the above components are mixed to form vesicles. Wherein, the contents of soybean lecithin and sodium cholate are as follows, the content of docetaxel is 0.2%, the content of ascorbyl palmitate is 0.1%, the content of vitamin E is 0.1%, and the content of ethanol is 20%.

[0039] The free drug and vesicles were separated by Sephadex G-50 gel, the encapsulation efficiency was detected by HPLC, and the particle size was measured by laser particle siz...

Embodiment 9～12

[0045] Soy lecithin (phosphatidylcholine > 92%) and a certain amount of docetaxel, active vitamin D 3 (Increase the anticancer effect of docetaxel activity) Dissolve with ethanol, after mixing evenly, remove ethanol by rotary evaporation, add 5mM phosphate buffer solution (pH 6.8) of sodium deoxycholate, add ethylene glycol, stir and sonicate at room temperature After 1 hour, a translucent preparation containing elastic nanovesicles was obtained, and the elastic nanovesicles were suspended in the mixed solution of various components remaining after the above components were mixed to form vesicles. Encapsulation efficiency and appearance are shown in Table 6. Among them, soybean lecithin 7%, active vitamin D 3 The content of docetaxel is shown in Table 5, the content of sodium deoxycholate is 1.5%, and the content of ethylene glycol is 20%.

[0046] Table 5 Docetaxel content

[0047] Sample No.

Docetaxel

1

0.1％

2

0.2％

3

...

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Abstract

The invention pertains to the technical field of medicine, which more particularly relates to an elastic nano-vesicle preparation used for transitting the active ingredient paclitaxel (taxol) or docetaxel to penetrate the natural permeability barriers or pores (such as, skin, mucosa, tissues and organs, etc.) and a preparation method thereof. The preparation at least contains the following components with the weight percentages: 3 to 15 percent of phospholipid, 0.3 to 5 percent of sodium cholate or sodium deoxycholate, 0.01 to 5 percent of paclitaxel or docetaxel, 5 to 30 percent of alcohol and the rest of water or phosphate buffer solution. The formed elastic nano-vesicle has lipid double molecular layers, and the diameter of the typical elastic nano-vesicle is less than 200nm. The preparation is used for the treatment of malignant tumors, and the invention can be taken by injection, spray or transdermal drug delivery.

Description

technical field [0001] The invention belongs to the technical field of medicine, and particularly relates to an elastic nanovesicle preparation and a preparation method thereof for transporting active ingredients paclitaxel (taxol) or docetaxel through natural permeable barriers or pores (such as skin, mucous membranes, tissues and organs, etc.). Background technique [0002] Taxine drugs are new anti-tumor drugs extracted or semi-synthesized from the bark or needles of Taxus chinensis. They act on the microtubule / tubulin system. Unlike other plant alkaloids, they promote the assembly of microtubule dimers. Microtubules, and stabilize microtubules by preventing the depolymerization process, arresting cells in G2 and M phases, thereby inhibiting mitosis and proliferation of cancer cells. At present, there are two kinds of drugs in clinical practice, paclitaxel and docetaxel. The former is a natural product isolated from yew, which was approved by the US FDA in 1992. The lat...

Claims

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Application Information

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IPC IPC(8): A61K31/337A61K9/127A61K9/00A61K47/24A61P35/00
Inventor 高云华邱玉琴胡科家徐百
Owner TECHNICAL INST OF PHYSICS & CHEMISTRY - CHINESE ACAD OF SCI
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