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Nanoparticle-loaded microsphere system for injection and preparation method of system

A nanoparticle and injection technology, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, and pharmaceutical formulas, can solve the problems of easy aggregation, instability, and poor sustained release of nanoparticles. To achieve the effect of enhanced sustained release, enhancement and controllability

Inactive Publication Date: 2013-06-05
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, both microspheres and nanoparticles have different degrees of defects
For example, the burst release effect of microsphere drugs is obvious, and the sustained release effect of some small molecule drugs is poor, while nanoparticles are easy to aggregate and unstable.

Method used

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  • Nanoparticle-loaded microsphere system for injection and preparation method of system
  • Nanoparticle-loaded microsphere system for injection and preparation method of system

Examples

Experimental program
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Effect test

Embodiment 1

[0044] Dissolve 100mg of BSA in 2ml of deionized water, adjust the pH to 9 with 0.1mol / l NaOH; dissolve 20mg of strychnine in 3ml of absolute ethanol, and add strychnine dropwise into the albumin solution while stirring rapidly After dispersing for 30 minutes, add 2ml of absolute ethanol solution dropwise for dehydration, add 1000ul of 0.25% glutaraldehyde aqueous solution, continue to stir and solidify for 10 hours, and remove the organic solvent by rotary evaporation at 35°C (35-40°C) . lyophilized. To prepare a 1% (v / v) acetic acid solution, dissolve CS in 0.5% (w / v) acetic acid. Brucine-BSA-Nps was added into the CS acetic acid solution at a ratio of 1:1 (BSA:CS) while stirring. Disperse for 1 hour, add 1% (v / v) glutaraldehyde (CS: glutaraldehyde) at a ratio of 10:1 while stirring, and cure for 1 hour. Spray dry. The air pressure is 40ml / h, the inlet temperature is 120°C, and the speed of the peristaltic pump is 20%.

Embodiment 2

[0046] Dissolve 100mg of BSA in 2ml of deionized water, and adjust the pH to 9 with 0.1mol / l NaOH; dissolve 20mg of cortisone in 3ml of absolute ethanol, and add nuxonum dropwise to the albumin solution while stirring rapidly Alkaline absolute ethanol solution, after dispersing for 30 minutes, continue to drop 2ml of absolute ethanol solution for dehydration, add 1000ul 0.25% glutaraldehyde aqueous solution, continue to stir and solidify for 10 hours, and remove the organic solvent by rotary evaporation at 35 ℃ (35-40). lyophilized. Weigh 36 mg of nanoparticles and dissolve in 200 μL of water as the inner water phase; in addition, take PLGA according to the ratio of excipients 1:1 (PLA:PGA=50:50, M r =6000) was dissolved in 4mL of dichloromethane as the oil phase, the probe was ultrasonicated, and after fully emulsified, 1% PVA solution was added at a ratio of 1:1 (PLGA:PVA), emulsified at a speed of 1000r / min for 3min, and the magnet was stirred at 500rpm for 1h. After stand...

Embodiment 3

[0048] Weigh 36 mg of hydrocortisone and dissolve it in 200 μL of water as the inner water phase; take another PLGA (PLA:PGA=50:50, M r =6000) 330mg dissolved in 4mL of dichloromethane as the oil phase, ultrasonic probe, after fully emulsified, add 1% PVA solution at 1:2 (PLGA:PVA), emulsify at 9000r / min for 3min, and stir at 500rpm for 1h , After standing still until the air bubbles in the table machine basically disappear, freeze-dry. To prepare a 1% (v / v) acetic acid solution, dissolve CS in 0.5% (w / v) acetic acid. The nanoparticles were added into the CS acetic acid solution with stirring at a ratio of 1:10 (PLGA:CS). Disperse for 1 hour, add 1% (v / v) glutaraldehyde at a ratio of 1:1 (CS: glutaraldehyde) while stirring, and cure for 1 hour. Spray dry. The air pressure is 40ml / h, the inlet temperature is 120°C, and the speed of the peristaltic pump is 20%.

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Abstract

The invention discloses a nanoparticle-loaded microsphere system for injection. Drugs are coated in nanoparticles, and the nanoparticles are coated in a microsphere, wherein the nanoparticles are made from material selected from one of albumin, chitosan and a polylactic acid-glycolic acid polymer, and the microsphere is made from either the chitosan or the polylactic acid-glycolic acid polymer. Furthermore, the invention provides a preparation method of the microsphere system, the nanoparticles are prepared through a desolvation and emulsification cross-linking method, a cross-linking method or a dual-emulsification method, and the prepared nanoparticles are further treated by the dual-emulsification method or a spray-drying method so as to obtain the microsphere. The nanoparticle-loaded microsphere system disclosed by the invention is free from a rejection reaction, and is applicable to parenteral administration; the microsphere system can adapt to natures of various drugs, which further enhances a controlled-release effect and controllability, the microsphere system can achieve a graded successive targeting effect by modifying two layers of materials inside and outside.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a nanoparticle-loaded microsphere system for injection and a preparation method thereof. Background technique [0002] The invention is a nanoparticle-loaded microsphere system for injection. Its main purpose is to wrap small molecule anti-inflammatory drugs such as strychnine, cortisone or hydrocortisone, and achieve the effect of treating arthritis through intra-articular injection. Purpose. [0003] The nanoparticle-loaded microsphere system is an emerging dosage form, mainly used as a carrier of genes or polypeptides. Mayank D. Bhavsar et al. used poly(ε-caprolactone) as a raw material and prepared a nanoparticle-in-microspheres oral system (NiMOS) by double emulsification method to deliver DNA to prevent DNA from being absorbed by the stomach. Intestinal digestion (Mayank D. Bhavsar, Mansoor M. Amiji, Gastrointestinal distribution and in vivo gene transfection st...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/19A61K47/42A61K47/36A61K47/34A61K31/475A61K31/573A61P19/02A61P29/00
Inventor 陈志鹏王建刘丹陈军蔡宝昌
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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