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PM (PTXPEG-PLA micelles)-coated nano-cluster and preparation method thereof

A kind of micellar nano-paclitaxel technology, which is applied in the direction of pharmaceutical formula, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of no increase in drug accumulation in tumor sites, shortened circulation time in the body, and nanoparticle particle size. In order to achieve the effect of reducing adverse reactions, increasing relative accumulation, and improving therapeutic effect

Active Publication Date: 2017-06-30
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, practice has shown that the compare did not increase the relative drug accumulation at the tumor site, but was slightly less than and internal circulation time compared to Shorten, can not provide enough time for paclitaxel to reach the tumor site to exert its curative effect
[0004] Studies have shown that solid tumors have an enhanced penetration and retention effect (EPR). Due to the relatively strong capillary permeability, the relative accumulation of nanoparticles in tumor tissue increases; however, the EPR effect has a certain effect on the particle size of nanoparticles. limit

Method used

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  • PM (PTXPEG-PLA micelles)-coated nano-cluster and preparation method thereof
  • PM (PTXPEG-PLA micelles)-coated nano-cluster and preparation method thereof
  • PM (PTXPEG-PLA micelles)-coated nano-cluster and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Weigh 50 mg PEG-PLA and 10 mg paclitaxel, add 4 ml acetonitrile, and ultrasonically dissolve the carrier material and drug fully. Place the solution in a rotary evaporator at 40°C for 30 minutes to evaporate the organic solvent to dryness, and place it in a vacuum oven overnight at room temperature to remove a small amount of residual solvent to obtain a dry and transparent drug film skeleton, then add 10ml of deionized water in the Stir at a constant speed of 500 rpm for 30 min, pass the hydration solution through a 0.22 μm cellulose acetate filter membrane to obtain a paclitaxel PEG-PLA micellar solution, add 0.5% PEI 200 μl to the paclitaxel PEG-PLA micellar solution under stirring at 500 rpm, Then 1ml of dichloromethane solution containing 20mgTPGS-CDI was added dropwise, the resulting emulsion was emulsified and ultrasonicated for 30min, and the organic solvent was removed by rotary evaporation at 40°C, 1mg IgG was added, and incubated at room temperature for 1h to ...

Embodiment 2

[0058] Weigh 70mg of PEG-PLA and 10mg of paclitaxel, add 4ml of dichloromethane, ultrasonically dissolve the carrier material and the drug, place the solution in a rotary evaporator at 40°C for 30min, and evaporate the organic solvent to dryness thoroughly. Put it in a vacuum drying oven overnight, remove a small amount of residual solvent to obtain a dry and transparent drug film skeleton, then add 10ml of normal saline and stir at a constant speed of 500rpm for 30min. Pass the hydration solution through a 0.22 μm cellulose acetate filter membrane to obtain a paclitaxel PEG-PLA micellar solution, add 200 μl of 0.5% PEI to the paclitaxel PEG-PLA micellar solution under stirring at 500 rpm, and add dropwise 1 ml containing 20 mg TPGS-CDI The resulting emulsion was emulsified and ultrasonicated for 30 min, and the organic solvent was removed by rotary evaporation at 30°C, 1 mg IgG was added, and incubated at room temperature for 1 h to prepare paclitaxel-encapsulated micellar nan...

Embodiment 3

[0060] Weigh 100mg PEG-PLA, 30mg paclitaxel, add 4ml dichloromethane, ultrasonically dissolve the carrier material and the drug, place the solution in a rotary evaporator at 50°C for 30min to evaporate the organic solvent thoroughly, and place in room temperature Put it in a vacuum drying oven overnight, remove a small amount of residual solvent to obtain a dry and transparent drug film skeleton, then add 15ml of normal saline and stir at a constant speed of 500rpm for 30min. Pass the hydration solution through a 0.22 μm cellulose acetate filter membrane to obtain a paclitaxel PEG-PLA micellar solution, add 0.5% PEI 300 μl to the paclitaxel PEG-PLA micellar solution under stirring at 500 rpm, and add dropwise 1 ml containing 20 mg PEG-CDI The resulting emulsion was emulsified and ultrasonicated for 30 min, and the organic solvent was removed by rotary evaporation at 40 °C, 1.5 mg of IgG was added, and incubated at room temperature for 1 h to prepare paclitaxel-encapsulated mice...

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Abstract

The invention belongs to the technical field of biological medicines, and relates to a PM (PTXPEG-PLA micelles)-coated nano-cluster and a preparation method thereof. The preparation method comprises the following steps of using an emulsifying ultrasonic method to prepare prepared PM into the PM-coated nano-cluster through a crosslinking agent; finally, adding hydrophilic micromolecules with negative charges to neutralize surface positive charges, and improving the hydrophilic property of a system. The PM-coated nano-cluster has the advantage that the PM is coated into a hydrophobic kernel of the micelles, so that on the basis of not influencing the higher drug carrying amount of the original micelles, the particle size of the system is effectively increased, the hydrophilic property of the system is improved, the circulating time in a human body is prolonged, the tumor EPR (enhanced permeability and retention) effect is enhanced, and the validity and safety of the medicine in the clinical application are improved.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to a paclitaxel-loaded micelle nanocluster and a preparation method thereof; the paclitaxel-loaded micelle nanocluster is a kind of drug that prolongs the circulation time of polymer micelles in vivo and effectively exerts the tumor EPR effect. Micellar nanoclusters for enhanced tumor therapy. [0002] technical background [0003] The prior art discloses that paclitaxel (PTX) is a first-line broad-spectrum anti-tumor drug, which can inhibit the mitosis process of tumor cells by promoting the polymerization of spindle tubulin, inhibiting depolymerization, and maintaining the stability of tubulin, thus playing an anti-tumor effect. , significant curative effect; but its solubility in water is less than 1ug / m. The paclitaxel listing preparation The PEG-PLA micelle system is mainly used to increase the dosage of paclitaxel. The amphiphilic material can form a copolymer micelle with...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/337A61K47/32A61K47/42
CPCA61K9/1075A61K31/337A61K47/22A61K47/32A61K47/34A61K47/42
Inventor 沙先谊梁慧慧
Owner FUDAN UNIV
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