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
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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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