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Triphenylphosphine-stearic acid grafted chitosan drug-loading micelle, and preparation and application thereof

A technology of triphenylphosphine and drug-loaded micelles, which is applied in the direction of pharmaceutical formulations, antineoplastic drugs, drug combinations, etc., can solve the problems of low curative effect, large toxic and side effects, etc., and achieve the goal of reducing toxic and side effects, reducing leakage, and increasing concentration Effect

Active Publication Date: 2018-02-09
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Limited by the physical and chemical properties of the drug molecule itself, the number of drug molecules that can enter the action site is very limited, which is the main reason for the large toxic side effects and low curative effect of existing drugs

Method used

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  • Triphenylphosphine-stearic acid grafted chitosan drug-loading micelle, and preparation and application thereof
  • Triphenylphosphine-stearic acid grafted chitosan drug-loading micelle, and preparation and application thereof
  • Triphenylphosphine-stearic acid grafted chitosan drug-loading micelle, and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] (1) Preparation of low molecular weight chitosan

[0035]Take 50g of chitosan with a molecular weight of 450kDa and a degree of deacetylation of 95%, add it to 1500mL of hydrochloric acid aqueous solution with a volume ratio of 1.2%, and stir for 2 hours at 55°C to fully swell the chitosan, then slowly add 2% chitosan enzyme solution, chitosan enzymolysis reaction is carried out under the condition of 55 ℃, and the degradation degree of chitosan is controlled by gel permeation chromatography. After the reaction is finished, stir at 80°C for 0.5 hour, add 0.3% active carbon in a weight / volume ratio, dilute the reaction solution, filter it with a Buchner funnel, and process the filtrate with a 0.45 μm microporous membrane, freeze-dry to a low Molecular weight chitosan, the weight average molecular weight of gained chitosan is 19.0kDa. Chitosan with a molecular weight of 450 kDa was degraded to 19 kDa and called low molecular weight.

[0036] (2) Synthesis of chitosan st...

Embodiment 2

[0042] (1) Preparation of low molecular weight chitosan

[0043] Take 50g of chitosan with a molecular weight of 450kDa and a degree of deacetylation of 95%, add it to 1500mL of hydrochloric acid aqueous solution with a volume ratio of 1.2%, and stir for 2 hours at 55°C to fully swell the chitosan, then slowly add 2% chitosan enzyme solution, chitosan enzymolysis reaction is carried out under the condition of 55 ℃, and the degradation degree of chitosan is controlled by gel permeation chromatography. After the reaction is finished, stir at 80°C for 0.5 hour, add 0.3% active carbon in a weight / volume ratio, dilute the reaction solution, filter it with a Buchner funnel, and process the filtrate with a 0.45 μm microporous membrane, freeze-dry to a low Molecular weight chitosan, the weight average molecular weight of gained chitosan is 19.0kDa.

[0044] (2) Synthesis of chitosan stearic acid graft

[0045] Take the above-mentioned chitosan with a molecular weight of 19.0 kDa, ad...

Embodiment 3

[0050] (1) Preparation of low molecular weight chitosan

[0051] Take 50g of chitosan with a molecular weight of 450kDa and a degree of deacetylation of 95%, add it to 1500mL of hydrochloric acid aqueous solution with a volume ratio of 1.2%, and stir for 2 hours at 55°C to fully swell the chitosan, then slowly add 2% chitosan enzyme solution, chitosan enzymolysis reaction is carried out under the condition of 55 ℃, and the degradation degree of chitosan is controlled by gel permeation chromatography. After the reaction is finished, stir at 80°C for 0.5 hour, add 0.3% active carbon in a weight / volume ratio, dilute the reaction solution, filter it with a Buchner funnel, and process the filtrate with a 0.45 μm microporous membrane, freeze-dry to a low Molecular weight chitosan, the weight average molecular weight of gained chitosan is 19.0kDa.

[0052] (2) Synthesis of chitosan stearic acid graft

[0053] Take the above-mentioned chitosan with a molecular weight of 19.0 kDa, ad...

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Abstract

The invention provides a triphenylphosphine-stearic acid grafted chitosan drug-loading micelle. The triphenylphosphine-stearic acid grafted chitosan drug-loading micelle is prepared through a two-stepamide method as follows: grafting tetracarboxybutyl triphenylphosphine to stearic acid grafted chitosan to obtain triphenylphosphine-stearic acid grafted chitosan having a mitochondrion targeting function; and performing coating of an antitumor drug amycin through a dialysis method to obtain the mitochondrion-targeting triphenylphosphine-stearic acid grafted chitosan drug-loading micelle. The drug-loading micelle provided by the invention has an efficient mitochondrion targeting function, and the coated drug amycin can maximally reduce the leakage of the amycin in normal tissues and non-target parts, thereby reducing the toxic or side effect; and meanwhile, a large amount of amycin can be accurately delivered to tumor cell mitochondria in a targeting manner, so that the concentration of the amycin in the tumor cell mitochondria is increased, apoptosis of the tumor cells is induced, and the antitumor curative effect is greatly improved.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to the construction of a mitochondria-targeted drug delivery system, in particular to the construction of a mitochondria-targeted triphenylphosphine-chitosan stearic acid graft drug-loaded micelle and its application in antitumor drugs application. Background technique [0002] Cancer has six major hallmarks which include: unlimited proliferative potential, insensitivity to growth inhibitory signals, inhibition of apoptosis, persistent proliferative signals, induction of angiogenesis, invasion and metastasis to other sites through capillary walls and basement membrane. Because cancer cells are mutations of normal cells, chemotherapeutic agents with the potential to kill cancer cells also produce nonspecific toxicity to normal tissues. [0003] Drug molecules act on the receptors, enzymes, and ion channels of the lesion cells mainly through the occupying effect. In recent years, the regulatio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00C08B37/08A61K9/107A61K31/704A61K47/36A61K47/34A61P35/00
CPCA61K9/1075A61K31/704A61K47/34A61K47/36C08B37/003C08G81/00
Inventor 胡富强孟廷廷袁弘谭亚南
Owner ZHEJIANG UNIV
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