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Tumor-targeted self-carrying system and preparation method and applications thereof

A tumor targeting and system technology, applied in the field of biomedicine, can solve the problems of low efficiency, no active targeting ability of apoptotic peptides, unsatisfactory tumor treatment effect, etc., to achieve convenient operation, good cell targeting ability, The effect of prolonging blood circulation time

Active Publication Date: 2019-05-03
智立中特(武汉)生物科技有限公司
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  • Abstract
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  • 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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  • Tumor-targeted self-carrying system and preparation method and applications thereof
  • Tumor-targeted self-carrying system and preparation method and applications thereof
  • Tumor-targeted self-carrying system and preparation method and applications thereof

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-targeted self-carrying system and a preparation method and applications thereof, and belongs to biomedicine. The tumor-targeted self-carrying system takes nano-micelleformed by amphiphilic apoptotic peptide as a carrier, entraps hydrophobic adriamycin in the nano-micelle, and binds hyaluronic acid outside the nano-micelle. The invention also provides a preparationmethod of the tumor-targeted self-carrying system: S1, synthesizing the amphipathic apoptotic peptide; S2, preparing an apoptotic peptide / adriamycin nano-micelle solution by using the amphipathic apoptotic peptide and the hydrophobic adriamycin; and S3, dissolving the hyaluronic acid in water, dropwise adding the obtained hyaluronic acid solution to the apoptotic peptide / adriamycin nano-micelle solution, performing standing, dialysis and centrifuging, and taking a supernatant to obtain a hyaluronic acid / apoptotic peptide / adriamycin nano-micelle solution, namely a tumor-targeted self-carryingsystem aqueous solution. The tumor-targeted self-carrying system of the invention is simple to prepare and high in drug loading amount, and has properties 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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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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