Oral composite nano-carrier based on cell-permeable peptide, preparation method and use thereof

A nano-carrier and membrane-penetrating peptide technology, applied in the field of medicine, can solve problems such as mucosal damage and clinical use restrictions, and achieve the effects of increasing local concentration, improving bioavailability, and promoting oral absorption

Inactive Publication Date: 2012-10-24
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The continuous use of common absorption enhancers will cause direct damage to the mucous membrane, which limits its clinical use

Method used

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  • Oral composite nano-carrier based on cell-permeable peptide, preparation method and use thereof
  • Oral composite nano-carrier based on cell-permeable peptide, preparation method and use thereof
  • Oral composite nano-carrier based on cell-permeable peptide, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Penetrating peptide modified 9-hydroxycamptothecin solid lipid nanoparticles

[0020] (1) Synthesis of penetrating peptides

[0021] Synthesis of SA-R by Solid Phase Synthesis 9 , the specific process is as follows:

[0022] Add 1g Rinkamide-MBHA resin (0.74mmol.g -1 ), add 20mL DMF to swell for 10min, and remove the solvent by suction filtration. Then 20 mL of 20% piperidine / DMF solution was added, stirred for 30 min, and suction filtered. The resin was washed 6 times with DMF, and the solvent was removed by suction filtration. Add 1.44g (2.22mmol) Fmoc-Arg(Pbf)-OH (Pbf is 2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl), 0.46g ( 2.22mmol) dicyclohexylcarbodiimide and 0.30g (2.22mmol) HOBt (1-hydroxybenzotriazole) and 20ml DMF, stirred at room temperature for condensation reaction. After 2 hours of reaction, a small amount of resin was taken for ninhydrin color reaction, and the result showed that the condensation reaction was complete. Suction filt...

Embodiment 2

[0028] Embodiment 2: Penetrating peptide modified paclitaxel solid lipid nanoparticles

[0029] (1) Synthesis of penetrating peptides

[0030] Synthesis of SA-R by Solid Phase Synthesis 8 , the specific process is as follows:

[0031] Add 1g Rinkamide-MBHA resin (0.74mmol.g -1), add 20mL DMF to swell for 10min, and remove the solvent by suction filtration. Then 20 mL of 20% piperidine / DMF solution was added, stirred for 30 min, and suction filtered. The resin was washed 6 times with DMF, and the solvent was removed by suction filtration. Add 1.44g (2.22mmol) Fmoc-Arg(Pbf)-OH (Pbf is 2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl), 0.46g ( 2.22mmol) dicyclohexylcarbodiimide and 0.30g (2.22mmol) HOBt (1-hydroxybenzotriazole) and 20ml DMF, stirred at room temperature for condensation reaction. After 2 hours of reaction, a small amount of resin was taken for ninhydrin color reaction, and the result showed that the condensation reaction was complete. Suction filtration, w...

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PUM

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Abstract

The present invention discloses a novel oral composite nano-carrier formed from a lipid cell-permeable peptide and solid lipid nanoparticles, a preparation method and a use thereof. According to the present invention, a film dispersion-ultrasound method is adopted to prepare solid lipid nanoparticles for drug loading; then a lipid cell-permeable peptide and the drug-loaded solid lipid nanoparticles are incubated to construct a novel oral composite nano-carrier. According to the composite nano-carrier of the present invention, a special absorption way of the solid lipid nanoparticles in gastrointestinal tract and an absorption promotion effect of the cell-permeable peptide are utilized so as to effectively solve the absorption problem of difficultly-absorbed oral drugs, and improve oral bioavailability of drugs.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and specifically uses membrane-penetrating peptide and solid lipid nanoparticles to construct a novel oral composite nanocarrier. The composite nano-carrier is characterized in that it utilizes the special absorption pathway of solid lipid nanoparticles in the gastrointestinal tract and the absorption-promoting effect of penetrating peptides to effectively solve the absorption problem of orally difficult-to-absorb drugs and improve the oral bioavailability of drugs. Background technique: [0002] Cell-permeable peptides (CPPs) are a class of polypeptides with strong cell membrane penetration ability, and they have the characteristics of efficiently passing through the cell membrane without damaging the structure and function of the cell membrane. Most studies have proved that penetrating peptides are basically non-toxic within the normal dosage range. Membrane-penetrating peptides can promote ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/42
Inventor 周建平吕慧侠张银龙张振海姜天玥孙博
Owner CHINA PHARM UNIV
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