Taxol-carried nano microbubble and preparation method thereof

A paclitaxel and microbubble technology, applied in the field of medical drugs, can solve the problems of intolerance by patients, large toxic and side effects, and achieve the effects of long duration, good stability, and increased cellular uptake of exogenous macromolecular substances

Inactive Publication Date: 2013-10-23
CHILDRENS HOSPITAL OF CHONGQING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the dissolution problem of paclitaxel has been solved, it is difficult for patients to tolerate due to the large toxic and side effects

Method used

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  • Taxol-carried nano microbubble and preparation method thereof
  • Taxol-carried nano microbubble and preparation method thereof
  • Taxol-carried nano microbubble and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] A paclitaxel-loaded nano-microbubble, the microbubble consists of a lipid bilayer membrane, containing N 2 , the lipid bilayer comprises a hydrophilic group and a hydrophobic group, the hydrophilic group links paclitaxel, and paclitaxel is loaded into the membrane formed by the lipid bilayer, and the lipid bimolecular The layer is composed of lecithin, cholesterol, PEG-4000, dextran, Span-80, methanol, ether, 3% HSA, paclitaxel standard substance, and PBS liquid. Its structure is as follows: figure 1 shown.

[0059] The preparation method of paclitaxel-loaded nano-microbubbles is carried out as follows:

[0060] (1) Put 0.1g lecithin and 0.04g cholesterol into the reaction bottle of the rotary evaporator, add ether to dissolve the lecithin and cholesterol; 40 ℃ water bath, the rotary evaporator works, see the bottom of the reaction bottle forms a layer of dry film to end the reaction , recover the ether into a bottle and keep it properly;

[0061] (2) configure 0.01...

Embodiment 2

[0067] A paclitaxel-loaded nano-microbubble, the microbubble consists of a lipid bilayer membrane, containing N 2 , the lipid bilayer comprises a hydrophilic group and a hydrophobic group, the hydrophilic group links paclitaxel, and paclitaxel is loaded into the membrane formed by the lipid bilayer, and the lipid bimolecular The layer is composed of lecithin, cholesterol, PEG-4000, dextran, Span-80, methanol, ether, 3% HSA, paclitaxel standard substance, and PBS liquid. Its structure is as follows: figure 1 shown.

[0068] The preparation method of paclitaxel-loaded nano-microbubbles is carried out as follows:

[0069] (1) Put 0.15g lecithin and 0.06g cholesterol into the reaction bottle of the rotary evaporator, add ether to dissolve the lecithin and cholesterol; 40 ℃ water bath, the rotary evaporator works, see the bottom of the reaction bottle forms a layer of dry film to end the reaction , recover the ether into a bottle and keep it properly;

[0070] (2) Configure 0.0...

Embodiment 3

[0076] A paclitaxel-loaded nano-microbubble, the microbubble consists of a lipid bilayer membrane, containing N 2 , the lipid bilayer comprises a hydrophilic group and a hydrophobic group, the hydrophilic group links paclitaxel, and paclitaxel is loaded into the membrane formed by the lipid bilayer, and the lipid bimolecular The layer is composed of lecithin, cholesterol, PEG-4000, dextran, Span-80, methanol, ether, 3% HSA, paclitaxel standard substance, and PBS liquid. Its structure is as follows: figure 1 shown.

[0077] The preparation method of paclitaxel-loaded nano-microbubbles is carried out as follows:

[0078] (1) Put 0.12g lecithin and 0.05g cholesterol into the reaction bottle of the rotary evaporator, add ether to dissolve the lecithin and cholesterol; 40 ℃ water bath, the rotary evaporator works, see the bottom of the reaction bottle forms a layer of dry film to end the reaction , recover the ether into a bottle and keep it properly;

[0079] (2) Configure 0.0...

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Abstract

The invention discloses a taxol-carried nano microbubble and a preparation method thereof. The microbubble has a membrane consisting of a lipoid bilayer and containing N2; the lipoid bilayer comprises hydrophilic groups and hydrophobic groups; the hydrophilic groups are bonded with taxol and the taxol is carried in the membrane consisting of the lipoid bilayer; and the lipoid bilayer is formed by compounding lecithin, cholesterol, polyethylene glycol (PEG)-4000, glucan, Span 80, methanol, ether, 3 percent human serum albumin, a taxol standard substance, and phosphate buffered saline (PBS) liquid. The taxol-carried nano microbubble does not have toxicity or side effect, can be used for peripheral intravenous injection, can pass through the lung and a capillary bed of the whole body (the diameter is generally less than 5 um), can be circulated to tissues of the whole body along with blood after the intravenous injection, has high stability, has a long duration in blood circulation, and does not influence blood flow dynamic of the whole body or a certain system.

Description

technical field [0001] The invention belongs to the field of medical medicine, and in particular relates to a paclitaxel-loaded nano-microbubble and a preparation method thereof. Background technique [0002] Restenosis often occurs after congenital or acquired vascular stenosis is treated by interventional surgery. The main pathological basis is the neointimal hyperplasia caused by the proliferation and migration of vascular smooth muscle cells. Paclitaxel, a microtubule inhibitor, has a stabilizing effect on microtubule dynamics, inhibits the normal formation of the spindle body, and inhibits transmembrane signal transduction and gene expression related to cell division, so its effect of blocking cell mitosis and proliferation is definite. Experiments have shown that paclitaxel can inhibit the division and proliferation of VSMCs, and can significantly reduce neointimal hyperplasia in restenosis models. [0003] Paclitaxel is white or off-white powder, highly fat-soluble,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K9/10A61K31/337A61P35/00
Inventor 计晓娟杨汝铃唐静
Owner CHILDRENS HOSPITAL OF CHONGQING MEDICAL UNIV
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