A tumor targeting self-carrier system and its preparation method and application

A tumor-targeting and systematic technology, applied in the field of biomedicine, can solve the problems of unsatisfactory tumor treatment effect, apoptosis peptide does not have active targeting ability, and low efficiency, so as to achieve good cell targeting ability and prolong blood circulation The effect of time and convenient operation

Active Publication Date: 2021-03-23
智立中特(武汉)生物科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, apoptotic peptides do not have active targeting ability, and the efficiency of enriching tumor sites only by passive targeting is low, resulting in unsatisfactory tumor treatment effects

Method used

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  • A tumor targeting self-carrier system and its preparation method and application
  • A tumor targeting self-carrier system and its preparation method and application
  • A tumor targeting self-carrier system and its preparation method and application

Examples

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Embodiment 1

[0050] Example 1 Synthesis of tumor targeting self-carrier system

[0051] (1) Synthesis of Amphiphilic Apoptotic Peptides

[0052] The amphipathic apoptosis peptide is formed by adding two N-fluorenylmethoxycarbonyl groups to the last lysine of the amino acid sequence shown in SEQ ID NO:1, which is D-lysine-leucine-alanine acid-lysine-leucine-alanine-lysine-lysine-leucine-alanine-lysine-leucine-alanine-lysine-glycine-cysteine Amino Acid-Lysine (N-Fremoxycarbonyl) 2 (KLAKLAKKLAKLAKGCK(Fmoc) 2 ).

[0053] Those skilled in the art can use solid-phase synthesis or liquid-phase synthesis to synthesize the above-mentioned amphipathic apoptosis peptide. In this application, the inventors synthesized it by solid-phase synthesis. The main steps are as follows:

[0054] 1) Weigh 1g of 2-chloro-trityl chloride resin (1.20mmol / g) into a clean solid-phase synthesis column, and swell the resin with 10mL N,N-dimethylformamide for 1.5h, then remove the synthetic resin by suction filtrati...

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Abstract

The invention relates to a tumor-targeting self-carrying system and its preparation method and application, belonging to biomedicine. The tumor-targeting self-carrying system uses nanomicelles formed by amphiphilic apoptosis peptides as carriers, Hydrophobic doxorubicin is contained inside, and hyaluronic acid is combined outside the nanomicelle. The present invention also provides the preparation method of the above-mentioned tumor targeting self-carrier system: S1. Synthesis of amphiphilic apoptosis peptide; S2. Preparation of apoptosis peptide / doxorubicin by using amphiphilic apoptosis peptide and hydrophobic doxorubicin Prime nano-micelle solution; S3. dissolve hyaluronic acid in water, add dropwise to the apoptosis peptide / doxorubicin nano-micelle solution, let it stand, centrifuge after dialysis and take the supernatant to obtain hyaluronic acid / adriamycin nano-micelle solution; The apoptosis peptide / doxorubicin nanomicelle solution is the aqueous solution of the tumor-targeting self-carrier system. The tumor-targeting self-carrier system of the invention is simple to prepare, has high drug loading capacity, and has the characteristics of excellent tumor targeting and high drug utilization rate.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a tumor-targeted self-carrier system and its preparation method and application. Background technique [0002] Tumor diseases have become one of the major diseases that threaten human health, and the incidence rate is increasing year by year, showing a trend of high morbidity, high mortality and younger age. It is imminent to realize effective treatment of tumor diseases. In order to effectively treat tumor diseases, in the past ten years, the construction of intelligent and delicate drug carriers has been attracting attention. However, the drug loading capacity of conventional drug carriers is not ideal, and generally less than 10%. , it is necessary to increase the dosage of drugs during the treatment process, and the increase of drug dosage will often cause serious side effects to patients. Therefore, it is urgent to construct a drug delivery system with high drug loading capacity w...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/42A61K47/36A61K31/704A61P35/00
Inventor 陈思樊锦轩鄢国平刘凡
Owner 智立中特(武汉)生物科技有限公司
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