Drug delivery system, and preparation method and application thereof

A delivery system and drug technology, applied in the field of nanomaterials, can solve the problems of low drug delivery efficiency and average drug delivery efficiency, and achieve the effect of long-term enrichment and high-efficiency delivery

Active Publication Date: 2018-02-02
艾赛普(广州)生物科技有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In response to these problems, the research and development and improvement of nanomaterials have made great progress in recent years, but the low drug delivery efficiency still exists.
According to a review report published in 2016 (Nature Reviews Materials 2016, 1, 16014), the average drug delivery efficiency of various nano drug delivery systems in vivo in the past 10 years is less than 0.7%.

Method used

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  • Drug delivery system, and preparation method and application thereof
  • Drug delivery system, and preparation method and application thereof
  • Drug delivery system, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0101] This embodiment prepares the polypeptide imaging agent (molecules of the structure shown in formula I) by the following method:

[0102] The molecule uses Cy7 as the functional molecule, the sequence of the molecular recognition part is AVPIAQK, the sequence of the substrate polypeptide of the response part is DEVD, the sequence of the polypeptide of the assembly part is KLVFFAECG, and the molecular structure and cleavage site are as follows: figure 1 As shown, the synthesis steps are as follows:

[0103] The Wang resin with a modification density of 0.35 mM was selected, the N-terminal of the first amino acid (lysine) was protected by Fmoc, and the C-terminal was fixed on the resin. The N-terminal Fmoc protection was removed with 20% hexahydropyridine solution in DMF, and then the deprotection result was detected by ninhydrin test. Then the carboxyl group of the next amino acid was treated with 0.4M N-methylmorpholine (NMM) and benzotriazole-N,N,N',N'-tetramethyluron...

Embodiment 2

[0122] In this embodiment, polypeptide drug molecules (molecules of the structure shown in formula II) are prepared by the following method:

[0123] The molecule uses Cy7 as a photothermal therapy drug, the target recognition sequence of the molecule is RGD, the responsive substrate polypeptide sequence is GPA, and the assembly polypeptide sequence is KLVFFGCG; the molecular structure and corresponding sites are as follows: Figure 7 As shown, the synthesis steps are as follows:

[0124] (1) Select Wang resin with a modification density of 0.35mM, protect the N-terminal of the first amino acid (lysine) by Fmoc, and fix the C-terminal on the resin. The N-terminal Fmoc protection was removed with 20% hexahydropyridine solution in DMF, and then the deprotection result was detected by ninhydrin test. Then the carboxyl group of the next amino acid was treated with 0.4M N-methylmorpholine (NMM) and benzotriazole-N,N,N',N'-tetramethyluronium hexafluorophosphate 10 times as much as...

Embodiment 3

[0130] This embodiment prepares the polypeptide imaging agent (molecules of the structure shown in formula I) by the following method:

[0131] The molecule uses Cy7 as the functional molecule, the sequence of the molecular recognition part is AVPIAQK, the sequence of the substrate polypeptide of the response part is DEVD, the sequence of the polypeptide of the assembly part is KLVFFAECG, and the molecular structure and cleavage site are as follows: figure 1 As shown, the synthesis steps are as follows:

[0132] The Wang resin with a modification density of 0.35 mM was selected, the N-terminal of the first amino acid (lysine) was protected by Fmoc, and the C-terminal was fixed on the resin. The N-terminal Fmoc protection was removed with 20% hexahydropyridine solution in DMF, and then the deprotection result was detected by ninhydrin test. Then the carboxyl group of the next amino acid was treated with 0.4M N-methylmorpholine (NMM) and benzotriazole-N,N,N',N'-tetramethyluron...

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Abstract

The invention discloses a drug delivery system, and a preparation method and an application thereof. The drug delivery system comprises a molecular recognition part, an assembling part, a response part, a functional molecule part and an optional long-circulation part, the assembling part is connected with the response part, the molecular recognition part is connected to the response part or the assembling part, the functional molecule part is connected to the side chain, far from the response part, in the assembling part, and the long-circulation part is connected with the response part. The drug delivery system prepared through the preparation method greatly improves the molecular delivery efficiency of a drug or an imaging agent, enhances the retention time in the lesion site, improves the enrichment efficiency of the drug or a contrast agent in the lesion site, improves the bioavailability of the drug, reduces the administration frequency, improves the safety of the drug, and provides a new drug delivery idea and technical way for the bottlnecks of the clinical transformation of nano-drugs.

Description

technical field [0001] The invention belongs to the field of nanomaterials, and relates to a drug delivery system and its preparation method and application. Background technique [0002] Supramolecular nano-drug delivery is an important part of nano-drug delivery, and some typical nanocarriers such as liposomes have been successfully used in clinical practice. However, supramolecular nano-drug delivery systems still face severe challenges, for example, their stability in complex physiological environments has been questioned due to their non-covalent composition. In addition, due to their different surface physical and chemical properties, size effects, shape effects, material composition, etc., different nano-delivery systems exhibit very different properties such as physiological interface interactions, metabolic pathways, and physiological toxicity. In response to these problems, the research and development and improvement of nanomaterials have made great progress in r...

Claims

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Application Information

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IPC IPC(8): A61K49/00A61K47/64A61K41/00A61P35/00
CPCA61K41/0052A61K49/0034
Inventor 王浩李莉莉安红维乔圣林
Owner 艾赛普(广州)生物科技有限责任公司
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