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Nano drug carrier targeting to central nervous system

A nano-drug carrier and central nervous system technology, applied in the field of medicine, can solve problems such as limited curative effect and serious side effects, and achieve the effect of targeted drug delivery

Active Publication Date: 2014-12-31
江苏申琅生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Nervous system diseases are a serious threat to human health. Although chemotherapy-based conventional treatment methods have achieved phased results in the past few decades, there are still problems such as limited curative effect and serious side effects.

Method used

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  • Nano drug carrier targeting to central nervous system
  • Nano drug carrier targeting to central nervous system
  • Nano drug carrier targeting to central nervous system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1. Preparation of alittin-polyethylene glycol-distearoylphosphatidylethanolamine at different modification sites

[0032] Take 0.2 μmol of Apamin (CNCKAPETALCARRCQQH-NH2) and dissolve it in freshly distilled dimethyl Incubate in formamide (DMF) at room temperature for 48 hours, put the resulting reaction mixture in a dialysis bag with a molecular weight of 3500 Da, dialyze with deionized water for 48 hours, and freeze-dry to obtain Apamin-PEG3400-DSPE.

[0033] Apamin (Fmoc-CNCKAPETALCA-RRCQQH-NH) protected by Fmoc (Fmoc-CNCKAPETALCA-RRCQQH-NH 2 ) 0.2μmol, dissolved in DMF, and then dissolved in freshly steamed DMF with NHS-PEG3400-DSPE according to the molar ratio of 1:1.2, incubated at room temperature for 48h, the reaction mixture was placed in a dialysis bag with a molecular weight of 3500Da, and deionized water was used as The medium was dialyzed for 48 hours and freeze-dried to obtain Fmoc-Apamin1-PEG3400-DSPE. Dissolve Fmoc-Apamin1-PEG3400-DSPE with 20%...

Embodiment 2

[0035] Example 2. Preparation and in vivo distribution test of drug-loaded nanomicelles with different modified sites of alittin-polyethylene glycol-distearoylphosphatidylethanolamine as targeting materials

[0036] 1. Preparation of drug-loaded nanomicelles

[0037] The near-infrared fluorescent dye DiR was used as a model drug. Mix Apamin-PEG3400-DSPE, Apamin1-PEG3400-DSPE, Apamin4-PEG3400-DSPE with mPEG2000-DSPE at a molar ratio of 10:90, dissolve in 0.5mL of chloroform, then add DiR methanol solution, mix well, 37℃ Evaporate under reduced pressure to form a thin film, dry in vacuum for 1.5h, then add 0.2mL of PBS (pH7.4), vortex for 10min, shake at 37°C for 1.5h, filter with a filter membrane with a pore size of 0.22μm, and then pass the filtrate through a micro homogenizer The drug-loaded nanomicelles Apamin-PEG-DSPE-DiR, Apamin1-PEG-DSPE-DiR, and Apamin4-PEG-DSPE-DiR with an average particle size of 50 nm were respectively prepared.

[0038] 2. In vivo distribution tes...

Embodiment 3

[0041] Example 3. Preparation and in vivo distribution test of drug-loaded nanomicelles with different particle sizes

[0042] 1. Preparation of drug-loaded nanomicelles

[0043] Mix Apamin-PEG3400-DSPE and mPEG2000-DSPE according to the molar ratio of 10:90, dissolve with 0.5mL of chloroform, then add DiR methanol solution, mix well, evaporate under reduced pressure at 37°C to form a film, dry in vacuum for 1.5h, then add PBS (pH7.4) 0.2mL, vortex for 10min, shake at 37°C for 1.5h, filter with a filter membrane with a pore size of 0.45μm, and the filtrate was homogenized by a micro-homogenizer to obtain average particle sizes of 50, 100, 200, 400nm drug-loaded nanomicelle Apamin-PEG-DSPE-DiR.

[0044] 2. In vivo distribution test

[0045] The SPD-grade Kunming mice were randomly divided into 4 groups, and the drug-loaded nano-micelle Apamin-PEG-DSPE-DIR with an average particle size of 50, 100, 200, and 400 nm was injected into the tail vein respectively. One mouse was ane...

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Abstract

The invention discloses a nano drug carrier targeting to a central nervous system. The nano drug carrier includes nano-micelles, nano-lipidosomes, nano-particles and the like, takes apamin or an apamin derivative exposed on the surface of the carrier as a targeting ligand, can carry a small-molecule chemical drug to cross blood brain barrier and blood spinal cord barrier, thereby realizing the central nervous system targeting drug administration, wherein the apamin derivative has a peptide chain C end without amidation.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a targeting nano drug carrier. Background technique [0002] Nervous system diseases are a serious threat to human health. Although chemotherapy-based conventional treatment methods have achieved phased results in the past few decades, there are still problems such as limited curative effect and serious side effects. For this reason, over the years, research on the pathogenesis, related targets and specific therapeutic drugs of neurological diseases has not stopped for a moment. Since the blood-brain barrier and the blood-spinal cord barrier are the main obstacles that prevent drugs from entering the central nervous system, it is of great significance to research and develop targeted drug delivery systems that can carry drugs through the blood-brain barrier and blood-spinal cord barrier. [0003] Apamin is a major polypeptide in bee venom, accounting for 3% of the dry weight of bee venom. I...

Claims

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Application Information

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IPC IPC(8): A61K47/42A61K47/34A61K9/16A61K9/51A61K9/127A61P25/00A61P25/28
Inventor 李翀吴瑾陈章宝
Owner 江苏申琅生物科技有限公司
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