Easily degradable responsive core-crosslinkable amphiphilic block polymer, preparation method thereof and application of amphiphilic block polymer as drug carrier

An amphiphilic block and easily degradable technology, which is used in medical preparations, pharmaceutical formulations, and emulsion delivery of non-active ingredients, can solve problems such as long-term toxicity, and achieve high drug loading, mild reaction conditions, and adverse reactions. less reactive effect

Pending Publication Date: 2021-07-13
XIANGTAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is worth noting that in most of the drug-loaded micelles of the existing research, the hydrophobic segment is composed of an alkyl segment, and its accumulation in human tissues and organs may cause long-term toxicity to the body, which may Degradable micelles are more conducive to in vivo applications, because biodegradable polymers are biodegraded in vivo by enzymatic or non-enzymatic means, and the by-products produced are biocompatible or harmless

Method used

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  • Easily degradable responsive core-crosslinkable amphiphilic block polymer, preparation method thereof and application of amphiphilic block polymer as drug carrier
  • Easily degradable responsive core-crosslinkable amphiphilic block polymer, preparation method thereof and application of amphiphilic block polymer as drug carrier
  • Easily degradable responsive core-crosslinkable amphiphilic block polymer, preparation method thereof and application of amphiphilic block polymer as drug carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Synthesis of polyethylene glycol monomethyl ether-b-polylactide block polymer mPEG-b-P(LA-SS-Py) containing dithiopyridine side groups and carboxyl side groups:

[0066] 1. Synthesis of ethyl hydroxydithiopyridine compound (HO-SS-Py):

[0067] Weigh DTDP (5g, 0.022mol) and 0.3mL of glacial acetic acid in a 50mL round-bottomed flask with a magnet, dissolve it completely with 25mL of methanol, and add dropwise to the mixture containing 2-mercaptoethanol (0.886 g, 11.36 mmol) in 5 mL of methanol solution, after the addition was completed, the reaction mixture was stirred at room temperature for 3 to 4 hours, then the stirring was stopped, and the solvent was evaporated to obtain the crude product of yellow oil, which was purified by silica gel column chromatography, Using silica gel as the stationary phase and a mixture of ethyl acetate / petroleum ether as the eluent, excess DTDP first appeared in a 15% ethyl acetate / petroleum ether mixture, then the polarity of the eluent ...

Embodiment 2

[0075] Preparation of micelles:

[0076] 1. Preparation and size adjustment of blank non-crosslinked micelles:

[0077] Take 10 mg of the amphiphilic block polymer obtained in Example 1 above, dissolve it in 4 mL of DMF, then add it dropwise to 6 mL of deionized water, stir for 4 h, transfer it to a dialysis bag (MWCO=3500 Da), and use Dialyze with deionized water, change the water every 3 hours, filter through a 0.45 μm filter membrane after 12 hours, freeze-dry, and finally obtain amphiphilic block copolymer blank non-crosslinked micelles. Figure 7 Middle a is the DLS diagram of the blank non-crosslinked micelles, the average particle size is 84nm, and the PDI is 0.126.

[0078] 2. Preparation of blank cross-linked micelles:

[0079] Take 10 mg of the amphiphilic block polymer obtained in Example 1 above, dissolve it in 4 mL of DMF, and then add it dropwise to a solution containing (30% relative to the dithiopyridine group) dithiothreose under a nitrogen atmosphere. Alco...

Embodiment 3

[0085] Micellar Stability Test:

[0086] Take the four kinds of micelles prepared in Example 2 and configure them into two parts of 1 mg / mL solution. At room temperature, dilute them by 3 times and 10 times with DMF solvent respectively. Distribution, after being diluted with the organic solvent DMF, the particle size changes, such as Figure 8 As shown, the particle size of the cross-linked micelles only increased slightly after being diluted 3 times and 10 times with DMF solvent, which indicated that it only swelled to a certain extent under the dilution of organic solvents, and there was no dissociation phenomenon, maintaining a relatively good stability. On the contrary, after the uncrosslinked micelles were diluted 3 times by DMF, larger particles appeared instead, which indicated that under the dilution of organic solvents, the uncrosslinked micelles dissociated and re-aggregated, while the diluted Uncrosslinked micelles were completely dissociated after ten times and ...

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Abstract

The invention discloses an easily degradable response type core-crosslinkable amphiphilic block polymer, a preparation method thereof and an application of the amphiphilic block polymer as a drug carrier. According to the amphiphilic block polymer, methoxypolyethylene glycol-b-polylactide serves as a main chain, and a side chain is modified with carboxyl and a dithiopyridine group; the amphiphilic block polymer and a water-insoluble drug can easily form a response type core cross-linked micelle, and the micelle is stable in a normal physiological environment, and is easy to be stimulated by environment after reaching tumour cells, and then, the cross-linked structure is damaged, so that the controlled release of the medicine is realized, the utilization rate of the medicine is improved, and the toxic and side effects of the loaded medicine are reduced; theamphiphilic block polymer is easy to degrade, so thatlong-term toxicity caused by accumulation of micelles in human tissues and organs is avoided; the amphiphilic block polymer has goodbiocompatibility, and has wide potential application prospects in the field of cancer chemotherapy; and the synthetic method of the amphiphilic block polymer is simple, mild in condition, few in side reaction and beneficial to expanded production.

Description

technical field [0001] The invention relates to a biopolymer material, in particular to an easily degradable core-crosslinkable amphiphilic block polymer, and to a preparation method for the easily degradable core-crosslinkable amphiphilic block polymer As well as its application as a water-insoluble drug delivery carrier, it belongs to the technical field of biomedical polymer materials. Background technique [0002] In modern society, surgical treatment, radiotherapy, and traditional chemotherapy are still the main methods of cancer treatment. Although traditional chemotherapy has been researched and developed for a long time, there are still problems that anticancer drugs are difficult to penetrate into the tumor, and long-term use produces drug resistance. Therefore, the targeted delivery and release of anticancer drugs has become one of the focuses of people's research on cancer treatment, and biodegradable polymeric micellar drug delivery systems with high therapeutic ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G63/664C08G63/91A61K47/34A61K9/107
CPCC08G63/664C08G63/912A61K9/1075A61K47/34
Inventor 张雪飞刘鸿辉李千蕊催力丹
Owner XIANGTAN UNIV
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