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A kind of sn-38 polymer micelle containing lipid and its preparation method and application

A polymer glue and polymer technology, applied in the field of medicine, can solve the problems of polymer modification complexity, unfavorable industrialization, safety issues, etc., and achieve high drug loading efficiency and stability, controllable quality, particle size even diameter effect

Active Publication Date: 2022-03-18
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] From the above studies, although chemical modification or covalent linking of SN-38 to polymers can improve its drug-loading efficiency to a certain extent, it still needs to be converted into active SN-38 by enzymes after entering the body. function, which is similar to CPT-11 and has the problem of conversion rate
In addition, the synthesis of new compounds itself is a relatively complicated process, which is time-consuming and not conducive to industrialization
From the perspective of chemical modification of the polymer itself, although the encapsulation efficiency of SN-38 has been improved, the reported results show that the drug loading is still low, which means that the polymer injected into the human body The amount of the object carrier will still be relatively high, so there are certain safety problems
Similarly, there is a certain complexity in the modification of polymers.

Method used

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  • A kind of sn-38 polymer micelle containing lipid and its preparation method and application
  • A kind of sn-38 polymer micelle containing lipid and its preparation method and application
  • A kind of sn-38 polymer micelle containing lipid and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0124] Embodiment 1: the preparation of the SN-38 polymer micelle containing HSPC

[0125] Weigh SN-385mg, HSPC 5mg, PEG 5k -PLA 8k 5 mg or 25 mg or 50 mg was placed in a 250 ml round bottom flask, fully dissolved with 6 ml of chloroform / methanol (9:1, v / v) mixed solvent to obtain a clear sample solution, and then rotated under reduced pressure at 25°C ( 2 mbar) to remove the organic solvent, and form a SN-38-lipid-polymer mixed film on the bottle wall, add 5ml ultrapure water at 40°C for 30 minutes, and then sonicate in an ice-water bath for 2 minutes to obtain SN-38 polymer containing HSPC micelle solution, take an appropriate amount of sample solution and centrifuge at 5000rpm for 10 minutes, take the supernatant and stock solution to measure the concentration of SN-38 by HPLC, and calculate the encapsulation efficiency according to the ratio of the two, the results are shown in figure 1 . The SN-38 polymer micelle solution containing HSPC prepared above is analyzed wit...

Embodiment 2

[0133] Embodiment 2: The influence of lipid content on the physical and chemical properties of SN-38 polymer micelles

[0134] Weigh SN-385mg, various types of lipids (such as DOTAP, DPPG, HSPC, EPC, DPPC) 0.01-20mg, PEG 5k -PLA 8k 50mg was placed in a 250ml round bottom flask, fully dissolved with 6ml of chloroform / methanol (9:1, v / v) mixed solvent to obtain a clear sample solution, and the organic solvent was removed by rotary evaporation under reduced pressure (2mbar) at 25°C , Form SN-38-lipid-polymer mixed film on the bottle wall, add 5ml ultrapure water to hydrate at 40°C for 30 minutes, then ultrasonicate in ice-water bath for 2 minutes to obtain SN-38 polymer micelle solution, take an appropriate amount of sample The solution was centrifuged at 5000rpm for 10 minutes, and the supernatant and stock solution were taken to measure the concentration of SN-38 by HPLC, and the encapsulation efficiency was calculated and determined according to the ratio of the two. The res...

Embodiment 3

[0148] Example 3: Effect of Lipid Type and Polymer Content on the Encapsulation Efficiency of SN-38 Polymer Micelles

[0149] Weigh 5 mg of SN-38, 5 mg of various types of lipids (such as DOTAP, DDAB, DOPG, DPPG, DSPC, HSPC, DPPC, DMPC, DLPC, MSPC, DOPC, EPC, DOPE, CHOL), PEG 5k -PLA 8k 12.5mg or 25mg or 50mg was placed in a 250ml round bottom flask, fully dissolved with 6ml chloroform / methanol (9:1, v / v) mixed solvent to obtain a clear sample solution, and then reduced pressure (2mbar) at 25°C Remove the organic solvent by rotary evaporation, and form a SN-38-lipid-polymer mixed film on the bottle wall, add 5ml ultrapure water at 40°C for 30 minutes, and then sonicate in an ice-water bath for 2 minutes to obtain SN-38 polymer micelles solution, take an appropriate amount of sample solution and centrifuge at 5000rpm for 10 minutes, take the supernatant and stock solution and use HPLC to measure the concentration of SN-38 respectively, calculate and measure the encapsulation ...

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Abstract

The present invention relates to a lipid-containing SN-38 polymer micelle and a preparation method and application thereof. The lipid-containing SN-38 polymer micelle is prepared from SN-38, lipid and an amphiphilic block copolymer, and the mass ratio of the SN-38 and the amphiphilic block copolymer is 1:1 -20, the mass ratio of the SN-38 to the lipid is 1:0.01-5; the lipid is selected from the group consisting of: phosphatidylcholine, phosphatidylethanolamine, phosphatidylglycerol, natural lecithin and cationic lipids At least one; the hydrophilic segment of the amphiphilic block copolymer is polyethylene glycol, and the hydrophobic segment of the amphiphilic block copolymer is selected from: polylactic acid, polyglycolic acid, polycaprolactone , Polyglycolide lactide, polyamino acid and derivatives. The lipid-containing SN-38 polymer micelles can significantly improve the encapsulation efficiency and stability of SN-38 in polymer micelles.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a lipid-containing SN-38 polymer micelle and its preparation method and application. Background technique [0002] SN-38 is a camptothecin derivative that selectively binds topoisomerase I (Top I) to inhibit DNA synthesis during cell division and induce cell death, thereby producing cytotoxic effects on cancer cells. SN-38 has extremely poor water solubility and cannot be administered directly in vivo. Its bipiperate prodrug irinotecan (CPT-11) is clinically used, which is approved by the FDA for colorectal cancer, small cell lung cancer, and pancreatic cancer Although ZCPT-11 and its liposome preparations have been widely used in the clinical treatment of various cancers, their anticancer activity is low, and they need to be metabolized into SN-38 to play a role in the body. The conversion rate is extremely low and there are obvious Individual differences lead to the unpredic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/24A61K47/34A61K31/4745A61K9/19A61P35/00
CPCA61K9/1075A61K47/24A61K47/34A61K31/4745A61K9/19A61K9/0019A61P35/00
Inventor 王均黄晓仪杨显珠杨艳芳李洁仪
Owner SOUTH CHINA UNIV OF TECH
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