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Preparation method of chitosan-loaded ciprofloxacin microsphere

The technology of chitosan and carrier ring is applied in the field of preparation of microsphere drug-carrying sustained-release system, which can solve the problems of poor bacteriostatic persistence and the like, and achieve the effects of good antibacterial properties, simple and easy operation, and excellent sustained-release performance.

Inactive Publication Date: 2020-12-29
NANJING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The antibacterial experiment of chitosan-loaded vancomycin microspheres prepared by emulsification and cross-linking method against Staphylococcus aureus showed that in the first 12 hours, the polylactic acid / chitosan nanocomposite fiber material could completely inhibit the growth of bacteria, but After that, the bacteria began to grow gradually and lasted for 20 days at most, and the antibacterial persistence was poor (Liu Wei et al. Preparation of vancomycin chitosan sustained-release microspheres and their in vitro drug release characteristics and antibacterial effects[J]. China Pharmacy, 2016 ,27(31):4443-4445.)

Method used

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  • Preparation method of chitosan-loaded ciprofloxacin microsphere
  • Preparation method of chitosan-loaded ciprofloxacin microsphere
  • Preparation method of chitosan-loaded ciprofloxacin microsphere

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Dissolve 0.4g of chitosan powder with a molecular weight of 100,000 in 40ml of 1% acetic acid solution, add ciprofloxacin according to the mass ratio of chitosan and ciprofloxacin at 1:1, fully dissolve, and then add 5ml of Span 80 was dissolved in 120ml of liquid paraffin and dissolved completely by ultrasonication respectively. Mix the two solutions and stir and emulsify for 30min under the conditions of stirring speed 500rmp and water bath 60°C, slowly add 5ml of 50% glutaraldehyde dropwise, continue stirring and crosslinking at 500rmp and water bath 60°C for 2h, and centrifuge the obtained suspension. The obtained precipitates were washed with petroleum ether and isopropanol, centrifuged several times, and the product was dried in an oven at 80° C., and then ground with a mortar to obtain the final product chitosan-loaded ciprofloxacin microspheres.

[0035] figure 2 It is the antibacterial effect diagram of 0.01 g of chitosan-loaded ciprofloxacin microspheres (ch...

Embodiment 2

[0037] Change the mass ratio of chitosan / ciprofloxacin in Example 1 to 2:1 and 4:1 respectively, and the other steps are the same as in Example 1. figure 1 It is a scanning electron microscope image of chitosan-loaded ciprofloxacin microspheres (chitosan: ciprofloxacin=4:1), wherein the magnification of image a is 7000, and the magnification of image b is 15000. It can be seen from the figure that the particle size of the microspheres is basically distributed between 1-5 μm, which is relatively uniform. The antibacterial effect of chitosan ciprofloxacin microsphere powder with different drug loading ratios on Staphylococcus aureus, image 3 Chitosan: ciprofloxacin = 2: 1, inhibition zone D = 40mm, Figure 4 Chitosan: ciprofloxacin = 4:1, antibacterial zone D = 36mm, it can be seen that with the decrease of the dose of ciprofloxacin, the antibacterial effect is gradually weakened.

Embodiment 3

[0039] This example is basically the same as Example 1, the only difference is that the volume ratio of liquid paraffin and acetic acid solution is 4:1. The SEM image of the prepared chitosan-loaded ciprofloxacin microspheres is as follows Figure 13 As shown, the spherical shape is good, the surface is relatively smooth, and there is less adhesion, which is no obvious difference compared with the 3:1 in Example 1.

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Abstract

The invention discloses a preparation method of a chitosan-loaded ciprofloxacin microsphere. The preparation method comprises the following steps: ultrasonically dissolving chitosan and ciprofloxacinhydrochloride in an acetic acid solution to obtain a solution 1, ultrasonically dissolving span-80 in liquid paraffin to obtain a solution 2, mixing the solution 1 and the solution 2 according to a volume ratio of the liquid paraffin to the acetic acid solution of 3:1-4:1 and a mass ratio of span-80 to chitosan of 25:2, performing stirring and emulsifying at 40-60 DEG C, slowly dropwise adding a glutaraldehyde solution, and performing stirring and cross-linking to obtain the chitosan-loaded ciprofloxacin microsphere. The chitosan-loaded ciprofloxacin microsphere prepared the method has a relatively smooth surface, and a particle size uniformly distributed between 1 [mu]m and 5 [mu]m, and has good antibacterial property and slow-release performance.

Description

technical field [0001] The invention belongs to the technical field of preparation of microsphere drug-loaded sustained-release systems, and relates to a preparation method of chitosan-loaded ciprofloxacin microspheres. Background technique [0002] Chitosan (CS) Chitosan is a natural polysaccharide that can be obtained by deacetylation of chitin, the chemical name is (1,4)-2-acetylamino-2-deoxy-β-D-glucan, The molecular chain is rich in amino groups and is widely used in the field of medicine. Compared with other natural polymers, chitosan is polycationic after protonation, has excellent biocompatibility, biodegradability and good mucoadhesion, and is widely used in the fields of medicine, food, textile and environmental protection. (Fang Chao. Preparation and drug-loading performance of chitosan / montmorillonite and chitosan / ferric oxide composite chitosan composite microspheres [D]. Guangzhou: South China University of Technology, 2015.). [0003] Ciprofloxacin has a wid...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K9/52A61K47/36A61K31/496A61P31/04A61L15/46A61L15/28
CPCA61K9/5036A61K31/496A61P31/04A61L15/46A61L15/28A61L2300/232A61L2300/404A61L2300/602C08L5/08
Inventor 江晓红徐沁李贝贝连瑞哲曹金星
Owner NANJING UNIV OF SCI & TECH
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