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Amphipathic segmented copolymer micelle compound drug loading and delivery system and preparation method of brain-targeted water-soluble micelle

A water-soluble glue, brain-targeting technology, which can be used in medical preparations without active ingredients, medical preparations containing active ingredients, drug combinations, etc. , reduce the problems of patient compliance, and achieve the effect of overcoming the easy resistance of single drugs, reducing the economic burden of patients, and reducing the single dose of administration.

Inactive Publication Date: 2017-05-24
SHANGHAI CHANGHAI HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the high price of the drug, the current use of lapatinib has greatly increased the toxic side effects and economic burden of cancer patients, and weakened the patient's compliance to a certain extent
[0007] For patients with advanced breast cancer, the side effects of the above drugs greatly reduce the compliance and greatly reduce the curative effect. The drug dosage form is basically ineffective against breast cancer brain metastases

Method used

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  • Amphipathic segmented copolymer micelle compound drug loading and delivery system and preparation method of brain-targeted water-soluble micelle
  • Amphipathic segmented copolymer micelle compound drug loading and delivery system and preparation method of brain-targeted water-soluble micelle
  • Amphipathic segmented copolymer micelle compound drug loading and delivery system and preparation method of brain-targeted water-soluble micelle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Example 1. Amphiphilic compound block nanomicelle 1# loaded with paclitaxel and lapatinib

[0058] A. Preparation stage: the amphiphilic compound block nano-micelle 1# loaded with paclitaxel and lapatinib involved in this embodiment one adopts such as figure 1 The preparation procedure shown was carried out.

[0059] In this example, the film hydration method was adopted, using methanol as the solvent, and the polymer malePEG-PLA was dissolved with lapatinib and paclitaxel, and the organic solvent was removed by rotary evaporation, and the film was dissolved in water with distilled water to form a carrier. The drug micelles were filtered to obtain pure water-soluble lapatinib-loaded nanomicelles.

[0060] The specific process steps are as follows:

[0061] Step 1. Dissolve 4mg lapatinib, 2mg paclitaxel and 40mg polymer malePEG-PLA together in 6ml of methanol (in the study, it was found that lapatinib could not reach the solubility required for the experiment in vario...

Embodiment 2

[0094] Example 2. Amphiphilic compound block nanomicelle 2# and brain-targeting nanomicelle loaded with paclitaxel and lapatinib

[0095] A. Preparation stage: The amphiphilic compound block nanomicelle 2# and brain-targeted nanomicelle loaded with paclitaxel and lapatinib involved in the second embodiment adopt such as Figure 4 The preparation procedure shown was carried out.

[0096] In Example 2, the thin-film hydration method was also used, using methanol as a solvent, and the polymers malePEG-PLA, COOH-PEG-PLA, paclitaxel and lapatinib were dissolved in methanol in proportion, and removed by rotary evaporation. Organic solvents and distilled water are used to dissolve the film in water to form drug-loaded micelles, and the covalent bonds formed by amino and carboxyl bonds are used to connect the micelles to the targeting molecule Angiopep-2 to prepare nano-carriers with brain-targeting functions. Drug micelles.

[0097] The specific process steps are as follows:

[00...

Embodiment 3

[0120] Example 3, Amphiphilic block nanomicelle 3# loaded with lapatinib

[0121] In Example 3, 4 mg of lapatinib, 2 mg of paclitaxel and 40 mg of polymer mPEG2000-PLA200 were dissolved in 6 ml of methanol; the mixed solution was transferred to a 250 ml eggplant-shaped bottle with a pipette. Under the condition of constant temperature water bath, remove the organic solvent by rotary evaporation, and obtain a light yellow film attached to the eggplant-shaped bottle; take off the eggplant-shaped bottle, use a pipette gun to absorb 4ml of distilled water, and dissolve the film completely under the condition of constant temperature water bath at 40°C in water to obtain light yellow transparent drug-loaded micelles; filter the obtained micelles to remove free drugs to obtain pure drug-loaded micelles.

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Abstract

The invention provides a brain-targeted water-soluble micelle. The brain-targeted water-soluble micelle is characterized in that a compound nano micelle loaded with paclitaxel and lapatinib is connected with a short peptide molecule Angiopep-2 of a cerebral endothelial cell. In the brain-targeted water-soluble micelle, the drug loading micelle having a brain-targeted function is prepared on the basis by preparing the compound water-soluble drug loading nano micelle. The molecule is connected with the targeted molecule Angiopep-2 by utilizing amidogen and carboxyl bonds, and the nano drug loading micelle having the brain-targeted function is prepared.

Description

technical field [0001] The invention relates to the field of brain-targeting preparations, in particular to an amphiphilic block copolymer micelle compound drug delivery system and a method for preparing brain-targeting water-soluble micelles. Background technique [0002] Taxanes (paclitaxel, docetaxel) are currently one of the main drugs for the treatment of metastatic breast cancer. Although taxanes are widely used, they have many unavoidable side effects, including: hair loss, fatigue, muscle pain , bone marrow suppression, neurotoxicity, allergic reactions, etc. [0003] At the same time, taxanes are highly insoluble in water, and their solubility in water is 0.5 μg / ml, so polyoxyethylene castor oil and absolute ethanol (1:1, V / V) should be used as cosolvents during administration. However, polyoxyethylene castor oil may induce fatal allergic reactions in patients. Therefore, in order to prevent allergic reactions, patients need to be pretreated with large doses of ant...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/64A61K47/69A61K47/34A61K31/517A61P35/04A61K31/337
CPCA61K9/0019A61K9/1075A61K31/337A61K31/517A61K47/34A61K2300/00
Inventor 王雅杰徐帅应明真庞志清曹师磊王一然
Owner SHANGHAI CHANGHAI HOSPITAL
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