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

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

Example Embodiment

[0031] Example 1. Preparation of melittin-polyethylene glycol-distearoylphosphatidylethanolamine with different modification sites

[0032] Take Apamin (CNCKAPETALCARRCQQH-NH2) 0.2μmol, and succinimide-polyethylene glycol 3400-distearoylphosphatidylethanolamine (NHS-PEG3400-DSPE) according to the molar ratio of 1:1.2 dissolved in freshly distilled dimethyl Incubate in formamide (DMF) for 48 h at room temperature, and place the resulting reaction mixture in a dialysis bag with a molecular weight of 3500 Da, dialyze for 48 h with deionized water as a medium, and lyophilize to prepare Apamin-PEG3400-DSPE.

[0033] Take Apamin (Fmoc-CNCKAPETALCA-RRCQQH-NH) with the N-terminal α-amino group of the peptide chain protected by Fmoc (fluorenyl methoxycarbonyl) 2 ) 0.2μmol, dissolved in DMF, and then dissolved with NHS-PEG3400-DSPE at a molar ratio of 1:1.2 in freshly steamed DMF, incubated at room temperature for 48h, the reaction mixture is placed in a dialysis bag with a molecular weight o...

Example Embodiment

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

[0036] 1. Preparation of drug-loaded nanomicelles

[0037] The near-infrared fluorescent dye DiR is used as a model drug. Mix Apamin-PEG3400-DSPE, Apamin1-PEG3400-DSPE, Apamin4-PEG3400-DSPE and mPEG2000-DSPE at a molar ratio of 10:90, dissolve with 0.5mL of chloroform, then add DiR methanol solution, mix well, 37℃ Evaporate into a thin film under reduced pressure, vacuum dry for 1.5 hours, add 0.2 mL of PBS (pH 7.4), vortex for 10 minutes, shake at 37°C for 1.5 hours, filter with a 0.22 μm filter membrane, and then pass the filtrate through a micro homogenizer. Evenly, the drug-loaded nanomicelles Apamin-PEG-DSPE-DiR, Apamin1-PEG-DSPE-DiR, and Apamin4-PEG-DSPE-DiR with an average particle size of 50nm were prepared.

[0038] 2. In vivo distribution test

[0039] The SPD...

Example Embodiment

[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, add DiR methanol solution, mix well, evaporate under reduced pressure at 37°C to form a film, vacuum dry for 1.5h, and add PBS (pH7.4) 0.2mL, vortex for 10min, shake at 37°C for 1.5h, filter with a 0.45μm pore size filter, the filtrate is homogenized by a micro homogenizer, and the average particle size is 50, 100, 200, 400nm drug-loaded nanomicelle Apamin-PEG-DSPE-DiR.

[0044] 2. In vivo distribution test

[0045] The SPD Kunming mice were randomly divided into 4 groups, and the drug-loaded nanomicelle Apamin-PEG-DSPE-DIR with an average particle size of 50, 100, 200, and 400 nm was injected into the tail vein respectively at 4 and 12 hours after administration. Take 1 mouse, anesthetize wit...

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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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