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Oral targeting nanoparticles based on intestinal epithelial cell apical OCTN2 transporter

A nanoparticle and stearyl technology, which is applied in the application field of oral drug carrier in drug delivery, can solve the problem that anti-tumor drugs cannot be taken orally, and achieve the effect of easy operation, good stability and high encapsulation efficiency

Active Publication Date: 2017-09-19
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a novel nano-drug delivery system targeting the intestinal OCTN2 transporter to solve the problem that the current anti-tumor drugs cannot be taken orally

Method used

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  • Oral targeting nanoparticles based on intestinal epithelial cell apical OCTN2 transporter
  • Oral targeting nanoparticles based on intestinal epithelial cell apical OCTN2 transporter
  • Oral targeting nanoparticles based on intestinal epithelial cell apical OCTN2 transporter

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Synthesis of Targeting Modifier L-Carnitine Derivatives

[0050] Add 3mmol (about 484mg) of L-carnitine and 3.6mmol of benzyl bromide into about 25ml of DMF, stir evenly, heat to 125°C, react under stirring conditions for 4 hours, distill off the solvent DMF and unreacted benzyl bromide under reduced pressure , That is, L-carnitine benzyl ester. Add 3mmol of stearic acid into about 15ml of dichloromethane and stir to dissolve, add 3.6mmol of oxalyl chloride dropwise, react for 0.5h under stirring conditions, distill off the solvent dichloromethane and unreacted oxalyl chloride under reduced pressure to obtain stearin acid chloride. Add the L-carnitine benzyl ester and stearyl chloride obtained above into about 25ml of acetonitrile and stir evenly, heat to 45°C, react under stirring conditions for 24h, remove the acetonitrile under reduced pressure, and use dichloromethane:methanol=19:1 The mobile phase is subjected to column separation to obtain stearoyl-L-carnitine b...

Embodiment 2

[0053] Preparation of ordinary PLGA NPs

[0054] Accurately weigh 0.50mg of paclitaxel (or coumarin 6), 10.0mg of PLGA, dissolve in 1mL of dichloromethane, mix it with 5mL of 1% PVA aqueous solution, sonicate for 5min with a power probe of 200w, stir at room temperature for 5h, The organic solvent was evaporated to obtain a nanoparticle solution. After centrifugation at 13000r / min for 30min, the supernatant was discarded, and deionized water was added to disperse. The operation was repeated three times, and the surfactant was washed away to obtain ordinary unmodified PLGA NPs.

Embodiment 3

[0056] Preparation of 5% LC-PLGA NPs

[0057] Accurately weigh 0.50 mg of paclitaxel (or coumarin 6), 0.50 mg of synthetic stearoyl-L-carnitine, and 10.0 mg of PLGA, dissolve them in 1 mL of dichloromethane, and mix them with 5 mL of 1% PVA aqueous solution Mix, ultrasonicate with 200w power probe for 5min, stir at room temperature for 5h, evaporate the organic solvent to obtain a nanoparticle solution, centrifuge at 13000r / min for 30min, discard the supernatant, add deionized water to disperse, repeat the operation three times, and wash off the surface active agent, that is, 5% LC-PLGA NPs.

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Abstract

The invention belongs to the field of new auxiliary materials and new dosage forms of pharmaceutic preparations, and relates to preparation of a derivative of L-carnitine as a substrate of an intestinal epithelial cell apical OCTN2 transporter and corresponding targeting nanoparticles, and application of the targeting nanoparticles as oral drug carriers in the aspect of drug delivery. Stearoyl-L carnitine is an amphipathic compound consisting L-carnitine as the substrate of the OCTN2 transporter and stearic acid, and is a targeting ligand which is good in stability and is used for constructing an OCTN2 targeting nano drug delivery system. The stearic acid can be long-chain fatty acids such as octadecanoic acid, palmitic acid and tetradecanoic acid. The structural formula of the amphipathic compound is as shown in the specification.

Description

technical field [0001] The invention belongs to the field of new excipients and new dosage forms of pharmaceutical preparations, and relates to the preparation of a derivative of L-carnitine, a substrate of OCTN2 transporter on the apical side of intestinal epithelial cells, and the corresponding targeting nanoparticles, and its use as an oral drug carrier applications in drug delivery. Background technique [0002] Nanotechnology has achieved rapid development in the 21st century, and the prospect of applying nanotechnology to drug delivery is very broad. Compared with conventional delivery systems, nanomedicine preparations have unique advantages such as small size effect, large specific surface area, and more functional groups or active centers linked or carried on the surface, making them suitable for sustained and controlled release, targeted drug delivery, and so on. It has shown obvious advantages in the fields of drug delivery, mucosal and local drug delivery, and p...

Claims

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Application Information

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IPC IPC(8): C07C227/18C07C229/22A61K9/51A61K47/32A61K47/18A61K45/00A61K31/337A61P35/00
CPCA61K9/5123A61K9/5153A61K31/337A61K45/00A61K47/186C07C51/60C07C227/16C07C227/18C07C229/22C07C53/42
Inventor 孙进何仲贵寇龙发
Owner SHENYANG PHARMA UNIVERSITY
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