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Silk fibroin nanoparticles and drug-loading silk fibroin nanoparticles

A technology of silk fibroin and nanoparticles, which is applied in the field of medicine, can solve the problems that drugs are difficult to reach the retinal therapeutic effect, low eye bioavailability, and large systemic side effects

Active Publication Date: 2017-09-15
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, the compliance of the systemic drug delivery route is high, but due to the obstruction of the blood-retinal barrier and the blood-brain barrier to the drug, only 1% to 5% of the drug can finally enter the vitreous body, and the bioavailability of the eye is extremely low, requiring repeated administration. Drugs that cause major systemic side effects
Most of the drugs administered by the periocular route are cleared by the capillaries of the conjunctiva and choroid, and the physiological barriers of the sclera, Bruch's membrane and retinal pigment epithelium make it difficult for the drugs administered by the periocular route to reach the retina to exert therapeutic effects

Method used

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  • Silk fibroin nanoparticles and drug-loading silk fibroin nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] 1. Preparation of silk fibroin nanoparticles

[0068] The silk fibroin material was dissolved in deionized water, stirred continuously until the silk fibroin was completely dissolved, and prepared into a silk fibroin solution with a concentration of 1.0% (w / v), and stood at 4° C. for 2 hours. Use a syringe to extract the above silk fibroin solution, and quickly inject it into a constant temperature ethanol solution at 60°C. The volume ratio (v / v) of ethanol to silk fibroin solution is 4:1. At the same time, use a magnetic stirrer to continuously stir the mixture until it forms Milky white nanoparticle suspension, continue to stir at constant temperature for 30 minutes. After the nanoparticles are completely formed, transfer the above nanosuspension to a centrifuge tube, centrifuge at 16,000 rpm for 30 min at 4°C, discard the supernatant, redisperse and wash the precipitate with deionized water, and centrifuge again to separate the nanoparticles, repeat This operation i...

Embodiment 2

[0077] 1. Preparation of silk fibroin nanoparticles

[0078] The silk fibroin material was dissolved in deionized water, stirred continuously until the silk fibroin was completely dissolved, and prepared into a silk fibroin solution with a concentration of 2.5% (w / v), and stood at 4° C. for 4 hours. Use a syringe to extract the above silk fibroin solution, and quickly inject it into acetone solution at a constant temperature of 40°C. The volume ratio (v / v) of acetone to silk fibroin solution is 6:1. Milky white nanoparticle suspension, continue to stir at constant temperature for 30 minutes. After the nanoparticles are completely formed, transfer the above nanosuspension to a centrifuge tube, centrifuge at 20,000 rpm for 30 min at 4°C, discard the supernatant, redisperse and wash the precipitate with deionized water, and centrifuge again to separate the nanoparticles, repeat This operation is performed 3 times. Finally, add quantitative deionized water to the above-mentioned...

Embodiment 3

[0087] 1. Preparation of silk fibroin nanoparticles

[0088] The silk fibroin material was dissolved in deionized water, stirred continuously until the silk fibroin was completely dissolved, and prepared into a silk fibroin solution with a concentration of 5.0% (w / v), and stood at 4° C. for 8 hours. Use a syringe to extract the above silk fibroin solution, and quickly inject it into isopropanol solution at a constant temperature of 20°C. The volume ratio (v / v) of isopropanol to silk fibroin solution is 8:1. At the same time, use a magnetic stirrer to continuously stir and mix solution until a milky white nanoparticle suspension is formed, and continue stirring at constant temperature for 30 min. After the nanoparticles are completely formed, transfer the above nanosuspension to a centrifuge tube, centrifuge at 4°C and 8000rpm for 30min, discard the supernatant, redisperse and wash the precipitate with deionized water, centrifuge again to separate the nanoparticles, repeat Thi...

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Abstract

The invention provides silk fibroin nanoparticles and drug-loading silk fibroin nanoparticles. The silk fibroin nanoparticles are prepared by a method comprising the following steps: dissolving silk fibroin in water, and keeping the water in which the silk fibroin is dissolved at 2-6 DEG C for 2-8h, so that a silk fibroin solution is obtained; mixing the silk fibroin solution with an organic solvent at the volume ratio of 1 to (4-8), and implementing stirring so as to obtain a nanoparticle suspension, wherein the organic solvent is selected from ethanol, isopropanol or acetone; implementing centrifugal separation on the nanoparticle suspension, washing the nanoparticle suspension by virtue of de-ionized water, and implementing centrifuging, so that a nanoparticle precipitate is obtained; and dispersing the nanoparticle precipitate by virtue of de-ionized water, so that the silk fibroin nanoparticles are obtained. The drug-loading silk fibroin nanoparticles can improve intake of drugs in cells and prolong retention time of the drugs; the drug-loading silk fibroin nanoparticles have the advantages of being effective, long-acting and targeted in cells and the drug-loading silk fibroin nanoparticles are conducive to the improvement of bioavailability of the drugs; the silk fibroin nanoparticles are excellent in biological adhesion and free from immunogenicity; and the silk fibroin nanoparticles are free from obvious inflammatory response and tissue fibrosis, and are excellent in biocompatibility and safety.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a silk fibroin nanoparticle and a drug-loaded silk fibroin nanoparticle. Background technique [0002] Neovascular diseases in the posterior segment of the eye mainly include age-related macular degeneration, retinopathy of prematurity and diabetic retinopathy, which are currently the main causes of vision loss and blindness in patients. The commonly used routes for the clinical treatment of neovascular diseases in the posterior segment of the eye include: systemic administration (such as oral and intravenous injection, etc.), periocular administration, and vitreous administration. Among them, the compliance of the systemic drug delivery route is high, but due to the obstruction of the blood-retinal barrier and the blood-brain barrier to the drug, only 1% to 5% of the drug can finally enter the vitreous body, and the bioavailability of the eye is extremely low, requiring repeate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/42A61K47/64A61K47/69A61K38/38A61P27/02
CPCA61K9/0051A61K9/5169A61K38/385
Inventor 朱春娥杨翩翩周奕先吴传斌黄迪
Owner GUANGDONG UNIV OF TECH
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