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A kind of pH-responsive enrofloxacin nanoparticle and its preparation method and application

A technology of enrofloxacin and nanoparticles, applied in the direction of pharmaceutical formulations, organic active ingredients, medical preparations of non-active ingredients, etc., can solve repeated drug administration, animal stress, increased drug side effects and drug-resistant bacteria Risks and other issues, to achieve excellent acid-responsive release profile, easy to obtain, acid-sensitive acid-triggered drug release characteristics

Active Publication Date: 2022-08-05
JIANGXI AGRICULTURAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, enrofloxacin is highly irritating to the gastrointestinal tract, easily causes animal stress during administration, and requires repeated administration many times during treatment
Ordinary enrofloxacin sustained-release preparations can reduce the irritation and dosing times of enrofloxacin, and achieve continuous dosing, but long-term low-dose administration may increase the risk of drug side effects and drug-resistant bacteria

Method used

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  • A kind of pH-responsive enrofloxacin nanoparticle and its preparation method and application
  • A kind of pH-responsive enrofloxacin nanoparticle and its preparation method and application
  • A kind of pH-responsive enrofloxacin nanoparticle and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Preparation of pH-responsive enrofloxacin nanoparticles (ENR-NPs)

[0038] (1) 1 mL of cinnamaldehyde was added dropwise to 20 mL of a 1% (v / v) acetic acid aqueous solution containing 0.2 g of chitosan, and stirred for 1 h to obtain a mixture containing cinnamaldehyde and chitosan;

[0039] (2) 2 mL of an anhydrous ethanol solution containing 30.1 mg of enrofloxacin was added dropwise to a mixture of 2 g of SPAN80 and 80 mL of liquid paraffin to obtain a mixture of enrofloxacin;

[0040] (3) The mixture containing cinnamaldehyde and chitosan was slowly added to the mixture containing enrofloxacin, and the pH of the solution was adjusted to 6.3 with 10% NaOH. After stirring at 40° C. for 3.5 hours, centrifugation at 12000 rpm for 30 minutes was performed to obtain a residue. ;

[0041] (4) The residue was repeatedly washed with petroleum ether and double distilled water for 5 times to obtain pH-responsive enrofloxacin nanoparticles (ENR-NPs);

[0042] (5) The ENR-NPs p...

Embodiment 2

[0044] Preparation of pH-responsive enrofloxacin nanoparticles (ENR-NPs)

[0045] (1) 1 mL of cinnamaldehyde was added dropwise to 20 mL of a 1% (v / v) acetic acid aqueous solution containing 0.2 g of chitosan, and stirred for 1 h to obtain a mixture containing cinnamaldehyde and chitosan;

[0046] (2) 2 mL of an anhydrous ethanol solution containing 29.9 mg of enrofloxacin was added dropwise to a mixture of 2 g of SPAN80 and 80 mL of liquid paraffin to obtain a mixture of enrofloxacin;

[0047] (3) The mixture containing cinnamaldehyde and chitosan was slowly added to the mixture containing enrofloxacin, and the pH of the solution was adjusted to 6.3 with 10% NaOH. After stirring at 40° C. for 3.5 hours, centrifugation at 12000 rpm for 30 minutes was performed to obtain a residue. ;

[0048] (4) The residue was repeatedly washed with petroleum ether and double distilled water for 5 times to obtain pH-responsive enrofloxacin nanoparticles (ENR-NPs);

[0049] (5) The ENR-NPs p...

Embodiment 3

[0051] Preparation of pH-responsive enrofloxacin nanoparticles (ENR-NPs)

[0052] (1) 1 mL of cinnamaldehyde was added dropwise to 20 mL of a 1% (v / v) acetic acid aqueous solution containing 0.2 g of chitosan, and stirred for 1 h to obtain a mixture containing cinnamaldehyde and chitosan;

[0053](2) 2 mL of an anhydrous ethanol solution containing 30.3 mg of enrofloxacin was added dropwise to a mixture of 2 g of SPAN80 and 80 mL of liquid paraffin to obtain a mixture of enrofloxacin;

[0054] (3) The mixture containing cinnamaldehyde and chitosan was slowly added to the mixture containing enrofloxacin, and the pH of the solution was adjusted to 6.3 with 10% NaOH. After stirring at 40° C. for 3.5 hours, centrifugation at 12000 rpm for 30 minutes was performed to obtain a residue. ;

[0055] (4) The residue was repeatedly washed with petroleum ether and double distilled water for 5 times to obtain pH-responsive enrofloxacin nanoparticles (ENR-NPs);

[0056] (5) The ENR-NPs pr...

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Abstract

The invention discloses a pH-responsive enrofloxacin nanoparticle and a preparation method and application thereof. The pH-responsive enrofloxacin nanoparticle is obtained by grafting chitosan and cinnamaldehyde to form a carrier and encapsulating the enrofloxacin. . The pH-responsive enrofloxacin nanoparticles prepared by the invention have an average drug encapsulation rate of 76.6% and a loading amount of 3.3%, have monodispersity, acid sensitivity and acid-triggered drug release characteristics, and due to their excellent Acid-responsive release profile and in vitro release, making it useful as a taste-masking agent for bacterial infection of DDS and bitter enrofloxacin. The cinnamaldehyde and chitosan used in the present invention are natural products with antibacterial activity, cheap and easy to obtain.

Description

technical field [0001] The invention belongs to the technical field of antibacterial drugs, and in particular relates to a pH-responsive enrofloxacin nanoparticle and a preparation method and application thereof. Background technique [0002] Enrofloxacin is a fluoroquinolone synthetic antibacterial agent, which is a widely used broad-spectrum antibiotic. It has a good preventive effect on common respiratory and intestinal bacterial diseases and mycoplasma in livestock and poultry. Its antibacterial mechanism is to inhibit bacterial DNA gyrase and topoisomerase IV, terminate bacterial DNA replication, transcription, repair and chromosome division of bacterial cell wall, thereby blocking bacterial DNA replication and achieve bacteriostatic purpose. The advantages of enrofloxacin are rapid antibacterial and bactericidal effect, excellent oral absorption and tissue distribution, small toxic and side effects, stable blood concentration, no cross-resistance with other antibiotics...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/36A61K47/08A61K47/02A61K31/496A61K31/722A61K31/11A61P31/04
CPCA61K9/5161A61K9/5123A61K9/5115A61K31/496A61K31/11A61K31/722A61P31/04A61K2300/00
Inventor 鲍光明杨俊岚袁厚群王立琦王小莺何嘉欣宋德平邓科
Owner JIANGXI AGRICULTURAL UNIVERSITY
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