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Improved preparation technology of alhumin nanosphere and inner ear transmembrane administration sustained release microsphere drug carrier

A slow-release microsphere preparation and serum albumin technology, applied in the direction of nano-medicine, nanotechnology, nanotechnology, etc., to achieve the effect of complete structure, large economic benefits, and uniform particle size

Inactive Publication Date: 2015-02-11
于湛
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far, there is no real slow-release preparation for local transmembrane drug delivery in the inner ear, and the use of serum albumin to prepare drug-loaded microspheres as a new type of drug carrier across the round window membrane has not been reported at home and abroad. Therefore the present invention has wide application prospect

Method used

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  • Improved preparation technology of alhumin nanosphere and inner ear transmembrane administration sustained release microsphere drug carrier
  • Improved preparation technology of alhumin nanosphere and inner ear transmembrane administration sustained release microsphere drug carrier
  • Improved preparation technology of alhumin nanosphere and inner ear transmembrane administration sustained release microsphere drug carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Take 50 mg of serum albumin and dissolve it in 10 mmol sodium chloride aqueous solution or double-distilled deionized water to obtain an aqueous solution containing serum albumin; add absolute ethanol solution under magnetic stirring, and the volume ratio of sodium chloride aqueous solution to absolute ethanol solution is 1:3 to 1:8, the addition rate of absolute ethanol is controlled at 1.0 to 3.0ml / min to form a milky white serum albumin suspension; put it in a water bath at 70°C for 30 minutes for thermal denaturation and curing, centrifuge, After drying, stable serum albumin blank microspheres are formed (see figure 1 a). The particle size distribution of the microspheres (see figure 1 b). Taking rhodamine B as a model drug and microspheres to blend and rely on physical adsorption to form a pink composite sustained-release microsphere carrier (see figure 2 a). The microspheres have stable physical and chemical properties, good repeatability, injectability and...

Embodiment 2

[0025] Dissolve 50mg of serum albumin blank microspheres in 5ml of PBS buffer and mix thoroughly, add 10mg of rhodamine B and incubate for 10min, put it into a special in vitro drug release chamber, and follow the sequence of every 1h, 4h, 8h, 12h, 24h, etc. Take out the liquid in the diffusion cell one by one, measure the absorption value at 560nm wavelength of the ultraviolet spectrophotometer, calculate the measurement of drug release according to the standard curve, calculate the cumulative drug release amount, and convert it into a percentage, that is, the percentage of cumulative released drug, the percentage of microspheres The in vitro release profile indicated that the cumulative release of the drug was 12% within one week. (See figure 2 d).

Embodiment 3

[0027] Take 50 mg of serum albumin and dissolve it in 10 mmol sodium chloride aqueous solution or double-distilled deionized water to obtain an aqueous solution containing serum albumin; add absolute ethanol solution under magnetic stirring, and the volume ratio of sodium chloride aqueous solution to absolute ethanol solution is 1:3 to 1:8, the addition rate of absolute ethanol is controlled at 1.0 to 3.0ml / min to form a milky white serum albumin suspension; put it in a water bath at 70°C for 30 minutes for thermal denaturation and curing, centrifuge, After drying, stable serum albumin blank microspheres are formed. Then, the cytotoxicity test (MTT method) was carried out, which indicated that the cell growth patterns of the control group and the experimental group were roughly the same through the solidification of heat-denatured serum albumin, and it could even be found that the cell growth state of the heat-denatured experimental group was better than that of the control bla...

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Abstract

A preparation method of inner ear trans round window membrane administration sustained release microsphere drug carrier involves inner ear transport of a series of drugs such as hormones, neurotrophic factors, free radical scavenger, aminoglycosides and intracranial antitumor drugs. The microsphere drug carrier can provide loading and transport of the above drugs, avoid the blood-brain barrier and blood labyrinth barrier and directly into the inner ear across the round window membrane and play a role through the tympanic membrane puncture technology, thereby greatly improving the effective local drug concentration of inner ear, while greatly reducing the toxicity and side effects caused by traditional systemic administration. The invention provides a sustained release microsphere preparation prepared from serum albumin and used for inner ear local drug administration and the preparation method thereof. The preparation method is as below: dissolving serum albumin in an aqueous solution containing sodium chloride or double distilled deionized water; adding anhydrous ethanol solution under magnetic stirring; carrying out water bath heat denaturation curing under high temperature, and centrifuging and drying to obtain the microsphere drug carrier; and blending the microsphere with rhodamine B as a model drug to form pink composite sustained release microsphere carrier preparation through physical adsorption.

Description

technical field [0001] The invention relates to a slow-release drug-loaded microsphere preparation for the treatment of inner ear diseases through the round window membrane transmembrane and its preparation process, and points out that it can carry a series of drugs such as hormones, neurotrophic factors, anti-free radicals, amino sugars Glycosides, intracranial anti-tumor drugs and other drugs. Background technique [0002] The clinical incidence of inner ear diseases (including cochlea and vestibular system) accounts for about 1 / 3 of otological diseases, such as sudden deafness, autoimmune inner ear disease and Meniere's disease, etc., which can lead to different degrees of sensory nerve damage. Deafness and balance dysfunction seriously affect the patient's working ability and quality of life. [0003] For a long time, systemic administration has been used to treat inner ear diseases clinically, among which glucocorticoids are one of the effective therapeutic drugs. Bec...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/42B82Y5/00A61P27/16
Inventor 于湛
Owner 于湛