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A drug targeted delivery carrier, preparation method and application thereof

A carrier and drug technology, applied in the direction of pharmaceutical formulations, drug combinations, anti-tumor drugs, etc., can solve the problems of non-targeted distribution, easy to be degraded during transportation, etc., and achieve stable shape and structure, complete protection, and good biocompatibility Effect

Active Publication Date: 2020-07-03
SHANGHAI ARGO BIOPHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the application of small interfering RNA technology also has the problems of non-targeted distribution in vivo, difficulty in introducing into cells, and easy degradation in blood transport.

Method used

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  • A drug targeted delivery carrier, preparation method and application thereof
  • A drug targeted delivery carrier, preparation method and application thereof
  • A drug targeted delivery carrier, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Preparation of folic acid-biotin-quaternized starch nanoparticles

[0043] The experimental principle is as follows,

[0044]

[0045] The specific preparation method is as follows:

[0046] a) preparation steps of quaternized starch:

[0047] 20 grams of potato starch is fully soaked in 12ml of isopropanol to form a starch isopropanol solution;

[0048] Dissolve 5.925 grams of NaOH in 8.24 grams of deionized water to form a NaOH solution, then pour 38.7 grams of 60% WT. etherification agent CTA into the NaOH solution, and stir at a high speed for 15 minutes to generate 2,3-epoxypropyl three Methyl ammonium chloride (GTA) solution;

[0049] Pour the generated 2,3-epoxypropyltrimethylammonium chloride (GTA) into the starch isopropanol solution at room temperature and stir at high speed for 1 hour to obtain a mixture, which is sealed and placed at 65°C React for 4 hours, cool to room temperature to generate white quaternized starch primary product, add anhydrous acet...

Embodiment 2

[0062] Preparation of folic acid-biotin-quaternized starch nanoparticles

[0063] The specific preparation method is as follows:

[0064] a) preparation steps of quaternized starch:

[0065] 20 grams of natural potato starch is fully soaked in 16ml of isopropanol to form a starch isopropanol solution;

[0066] Dissolve 5.925 grams of NaOH in 8.24 grams of deionized water to form a NaOH solution, then pour 38.7 grams of 60% WT. etherification agent CTA into the NaOH solution, and stir at a high speed for 15 minutes to generate 2,3-epoxypropyl three Methyl ammonium chloride (GTA) solution;

[0067] Pour the generated 2,3-epoxypropyltrimethylammonium chloride (GTA) into the starch isopropanol solution at room temperature and stir at high speed for 1 hour to obtain a mixture, which is sealed and placed at 65°C React for 4 hours, cool to room temperature to generate white quaternized starch primary product, add anhydrous acetic acid to neutralize to pH 6-8, then wash the quatern...

Embodiment 3

[0074] Preparation of folic acid-biotin-quaternized starch nanoparticles

[0075] The specific preparation method is as follows:

[0076] a) preparation steps of quaternized starch:

[0077] 20 grams of natural potato starch is fully soaked in 20ml of isopropanol to form a starch isopropanol solution;

[0078] Dissolve 5.925 grams of NaOH in 8.24 grams of deionized water to form a NaOH solution, then pour 38.7 grams of 60% WT. etherification agent CTA into the NaOH solution, and stir at a high speed for 15 minutes to generate 2,3-epoxypropyl three Methyl ammonium chloride (GTA) solution;

[0079] Pour the generated 2,3-epoxypropyltrimethylammonium chloride (GTA) into the starch isopropanol solution at room temperature and stir at high speed for 1 hour to obtain a mixture, which is sealed and placed at 65°C React for 4 hours, cool to room temperature to generate white quaternized starch primary product, add anhydrous acetic acid to neutralize to pH 6-8, then wash the quatern...

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Abstract

The invention discloses a targeted drug delivery carrier and a preparation method and application thereof; the targeted drug delivery carrier has a following structure shown in the description. Compared with the prior art, the targeted drug delivery carrier has zero toxicity, good biocompatibility and good form stability, can easily penetrate tumor tissues, and can effectively entrap hydrophobic antitumor drugs owing to its high drug-loading capacity and high entrapment efficiency. Through electrostatic adsorbing action of cation groups of quaternized starch and phosphate groups on siRNA, the siRNA is entrapped effectively, and the integrity of the siRNA is effectively protected in blood. The drug and siRNA co-carrier can provide active targeted delivery for tumor tissues; drug and siRNA co-carrier nano particles can stay in tumor tissues for a long time to release the drug and siRNA for a long time, can provide the joint therapy of tumor tissues by the drug and siRNA, with toxic and side effects on normal tissues relieved.

Description

technical field [0001] The invention belongs to a drug carrier, a preparation method and an application thereof, in particular to a chemotherapeutic drug and a small-molecule interfering RNA co-delivery carrier, a preparation method and an application thereof. Background technique [0002] Chemotherapy has always been the main means of cancer treatment, but the non-targeted dispersion of chemotherapeutic drugs in the body makes the drugs act on tumor tissues while damaging other normal tissues and organs in the body, resulting in a variety of side effects of chemotherapy. The characteristics of multidrug resistance make the clinical efficacy of chemotherapy unsatisfactory. The multidrug resistance of tumor cells is mainly reflected in the energy-dependent drug efflux pump on the cell membrane, which can pump the small molecule drugs entering the cell membrane out of the membrane, and the anti-apoptosis mechanism of tumor cells, which inhibits the tumor cell growth rate. Nor...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/54A61K47/69A61K31/7088A61P35/00A61K31/704
CPCA61K31/704A61K31/7088A61K2300/00
Inventor 龚仁敏李良萍宋明明张越陈款明王慧
Owner SHANGHAI ARGO BIOPHARMACEUTICAL CO LTD
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