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Nano drug delivery system for co-entrapping siRNA and hydrophobic drug, and preparation method and application thereof

A hydrophobic drug and nano-drug-loading technology, which can be used in drug combinations, pharmaceutical formulations, medical preparations with inactive ingredients, etc., can solve the problem of difficult co-transportation to tumor sites, etc. The effect of uniform particle size

Pending Publication Date: 2022-01-18
XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In view of the above background, the object of the present invention is to provide a nano-drug loading system co-encapsulating siRNA and hydrophobic drugs, its preparation method and application, which can co-deliver hydrophobic drugs FX and SiRNA to tumor targets, so as to solve the current problem Some FX and SiRNA are difficult to co-deliver to the tumor site

Method used

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  • Nano drug delivery system for co-entrapping siRNA and hydrophobic drug, and preparation method and application thereof
  • Nano drug delivery system for co-entrapping siRNA and hydrophobic drug, and preparation method and application thereof
  • Nano drug delivery system for co-entrapping siRNA and hydrophobic drug, and preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0050] Preparation of hydroxyethyl starch coupled cholesterol polymer (HES-CH), synthesized according to the following steps:

[0051] Step 1, amination of hydroxyethyl starch (HES)

[0052] Blend 1g of bromopropylamine hydrobromic acid with 1g of hydroxyethyl starch, add 2mL of sodium hydroxide solution with an equivalent concentration of 3.08N, react at 4°C for 20 minutes, add 37% concentrated hydrochloric acid to adjust the pH value to 7, The aminated hydroxyethyl starch (HES-NH2) is obtained, and the aminated hydroxyethyl starch (HES-NH2) is dialyzed to remove impurities, and then freeze-dried to obtain purified aminated aminated hydroxyethyl starch (HES-NH2) powder.

[0053] Step 2, dissolving 1g of cholesterol and 1g of succinic anhydride in 20ml of pyridine. The mixture was heated to 60°C and stirred for 3 hours, then dried by rotary evaporation to obtain a precipitate, which was dissolved in ethanol, and the white precipitate was obtained by rotary evaporation as carb...

Embodiment 2

[0059] Preparation of hydroxyethyl starch-coupled cholesterol nano drug delivery system:

[0060] Dissolve the purified hydroxyethyl starch-coupled cholesterol polymer (HES-CH) into water, use a sonicator, and add FX dichloromethane solution while sonicating in an ice bath, sonicate for 5 min, and the sonication ends Finally, the emulsion was added to a high-pressure homogenizer, and homogenized twice at 500 bar to obtain a suspension of FX@HES-CH and FX, which was then centrifuged at 5000 rpm for 30 min to remove unencapsulated FX, and part of FX@HES-CH The CH solution was placed in a 3500Da dialysis bag, and the siRNA aqueous solution was added to stir with FX@HES-CH for 0-120min. The mass ratio of siRNA to FX@HES-CH was 0.01:1-100:1, and then the suspension was added to Ultrafiltration tubes with a molecular weight of 3-15w were centrifuged at 5000rpm-15000rpm for 30min to obtain purified siRNA / FX@HES-CH nanoparticles co-loaded with siRNA and FX. Weigh the siRNA / FX@HES-CH ...

Embodiment 3

[0064] The pH-sensitive drug release behavior of HES-CH was studied.

[0065] Firstly, 1 mg / mL HES-CH nanoparticles were placed in pH 7.4, pH 6.8 and pH 5.4 environments for 30 min, and DLS was used to measure the particle size distribution of HES-CH nanoparticles in different pH states.

[0066] The result is as image 3 As shown, as the pH decreased, the particle size of HES-CH nanoparticles increased correspondingly. The dialysis bag method was used to test the release behavior of FX@HES-CH at different pHs. 0.5 mL of the suspension of FX@HES-CH nanoparticles (FX concentration 2.0 mg / mL) was placed in a dialysis bag (MWCO: 3500 Da), The dialysis bag was placed in 50.0 mL of release medium with different pH (5.4, 6.8, 7.4), 1 mL of release medium was taken out at different time points for quantitative analysis, and 1 mL of new medium was added at the same time.

[0067] The released amount of FX was measured by UV spectrophotometer (quantitative determination wavelength: 4...

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Abstract

The invention relates to a nano drug delivery system for co-encapsulating siRNA and a hydrophobic drug, and a preparation method and application thereof. According to the invention, nanoparticles co-encapsulating the hydrophobic drug and the siRNA are prepared by coupling hydroxyethyl starch and cholesterol with good biocompatibility, and the nanoparticles have pH-sensitive FX drug release capability, are uniform in particle size, stable in structure and good in biocompatibility, have the characteristics of multiple drug loading types and high stability when being compared with common nano carriers such as liposomes and micelles, can effectively deliver FX and the siRNA to the breast cancer site in a targeting mode so as to inhibit the growth of the breast cancer, and can inhibit the metastasis of the breast cancer and achieve the effect of the FX and the siRNA synergistic treatment on the triple negative breast cancer.

Description

Technical field: [0001] The invention belongs to the technical field of nano-biomedicine, and in particular relates to a nano-drug loading system for co-encapsulating siRNA and hydrophobic drugs, its preparation method and application. Background technique: [0002] At the present stage of cancer treatment, it is difficult to meet the clinical needs only with a single chemotherapy, such as triple negative breast cancer (Triplenegative breast cancer, TNBC), as the most aggressive subtype of breast cancer, about 46% of TNBC patients are diagnosed at the first stage after diagnosis. Distant metastases to lung, bone, brain and other organs occurred within three years. The median survival after transfer was only 13.3 months. The main treatment methods for clinical TNBC are traditional chemotherapy and surgery. Chemotherapy is the only systemic treatment available. For patients with locally recurrent inoperable or metastatic TNBC. However, under conventional chemotherapy, the ...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/336A61K31/337A61K31/7088A61K47/36A61P15/14A61P35/00A61P35/04C08B31/12
CPCA61K9/5161A61K31/7088A61K31/336A61K31/337A61P35/00A61P35/04A61P15/14C08B31/125A61K2300/00
Inventor 胡豫徐戎唐宇翔吴泽亮陈钊钊
Owner XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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