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Nano drug delivery system of equisetin and derivative thereof as well as preparation and application of nano drug delivery system in skin soft-tissue infection

A technology of iklamycin and nano-drug loading, which is applied in the field of pharmaceutical preparations in medical technology, and can solve the problems of repeated skin infection, difficulty in eradication, and difficulty in recovery

Inactive Publication Date: 2018-03-16
THE THIRD AFFILIATED HOSPITAL INST OF FIELD SURGERY OF PLA ARMY MEDICAL UNIV
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  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Staphylococcus aureus is the main pathogenic bacterium that causes purulent infection of skin and soft tissue. The skin disease caused by it can lead to continuous and repeated skin infection, which is difficult to heal, and it exists in the environment for a long time and is not easy to eradicate

Method used

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  • Nano drug delivery system of equisetin and derivative thereof as well as preparation and application of nano drug delivery system in skin soft-tissue infection
  • Nano drug delivery system of equisetin and derivative thereof as well as preparation and application of nano drug delivery system in skin soft-tissue infection
  • Nano drug delivery system of equisetin and derivative thereof as well as preparation and application of nano drug delivery system in skin soft-tissue infection

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Experimental program
Comparison scheme
Effect test

Embodiment -1

[0034] The anti-MRSA activity screening of embodiment-1 equisetin (equisetin) and epi-equisetin (epi-equisetin)

[0035] Anti-MRSA activity screening was performed using the K-B disc diffusion method. The specific steps are: a) activate MRSA; b) cultivate to the logarithmic phase; c) melt the sterilized MHA medium, let it cool to about 50°C, it is better not to burn the back of the hand; d) add an appropriate amount of MRSA in the logarithmic phase Put the bacterial solution into the melted sterilized MHA medium to a final concentration of about 106 / mL; e) Pour the plate while it is hot; f) Add 10, 18, 25ug of drug-containing filter paper and incubate at 30°C for 16 hours to observe the inhibition zone . Screening results showed that 1 (Iquimycin) had a strong antibacterial activity, followed by 2 (Epiquimycin). For specific results, see figure 1 .

Embodiment 2

[0036]Example 2 Spectrum Data Arrangement and Identification of Equisetin and Epi-Equisetin (See Figure 2)

[0037] Compound 1 equisetin(+)-HR-ESI-MS m / z:374.2328([M+H]+,calcd forC22H32NO4,374.2326);1H NMR(CDCl3 500MHz)δ:3.28(1H,brd,H -3),5.34(1H,brs,H-4),5.34(1H,brs,H-5),1.90(1H,brs,H-6),0.83,1.76(2H,m,H-7), 1.48(1H,m,H-8),1.08,1.69(2H,H-9),0.95,1.80(2H,m,H-10),1.62(1H,m,H-11),1.38(3H, brs, H-12), 5.13 (1H, m, H-13), 5.18 (1H, m, H-14); 1.47 (3H, brs, H-15), 0.85 (3H, d, J=7Hz, H-16), 3.56 (1H, brs, H-5'), 3.87, 3.91 (2H, d, J=14Hz, H-6'), 3.0 (3H, brs, H-7'), 13C NMR ( CDCl3, 125MHz) δ: 190.3(C-1), 48.7(C-2), 45.0(C-3), 126.9(C-4), 130.8(C-5), 38.5(C-6), 42.1( C-7), 33.2(C-8), 35.6(C-9), 28.2(C-10), 39.8(C-11), 14.0(C-12), 129.9(C-13), 126.5(C -14),17.7(C-15),22.3(C-16),177.0(C-2'),100.1(C-3),198.7(C-4'),67.3(C-5'),60.1 (C-6'),27.2(C-7');

[0038] Compound 2 epi-equisetin(+)-HR-ESI-MS m / z:374.2331([M+H]+,calcdfor C22H32NO4,374.2326);1H NMR(CDCl3 500MHz)δ:3.26(1H, brd,...

Embodiment 3

[0039] The nanoemulsion preparation of embodiment 3 equisetin (equisetin)

[0040] Nanoparticles were prepared by coating equisetin with BSA (bovine serum albumin). The specific method is to weigh 100 mg of BSA (bovine serum albumin) and dissolve it in double distilled water as the water phase, and simultaneously weigh 21 mg of equisetin and dissolve it in CHCl3:CH2OH (1:1) as the organic phase. Then the organic phase was slowly added to the water phase in the ice bath, and ultrasonicated in a sonicator at 60% power for 12 min. Finally, use a rotary evaporator to concentrate under reduced pressure to remove the organic solvent, and obtain equisetin albumin nanoparticles. Finally, the particle size, PDI, and Zeta potential of the nanoemulsion are tested and observed with a transmission electron microscope. It can be seen from the figure that equisetin The particle size of equisetin albumin nano-emulsion is about 230nm, and the distribution of nano-particle size is uniform, and...

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Abstract

The invention relates to a novel multifunctional nano drug delivery system of MRSA (Methicillin-Resistant Staphylococcus Aureus) equisetin and a derivative thereof as well as a preparation and application of the nano drug delivery system in skin soft-tissue infection MRSA, with the combination of nano techniques and electrostatic spinning techniques, nano electrostatic spinning yarns which are applied to skin soft-tissue infection and have the advantages of being large in specific surface area, high in porosity, good in air and moisture permeability and the like are prepared from the nano drugdelivery system, and a novel clinical treatment scheme is provided for skin soft-tissue infection MRSA. By adopting the nano drug delivery system, not only are problems of drug delivery systems for treating skin soft-tissue infection MRSA of MRSA equisetin and the derivative thereof solved, but also the bioavailability of medicines is improved, dual slow release is achieved, and the nano drug delivery system can be applied to treatment on skin soft-tissue infection.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations of medical technology, and relates to a novel multifunctional nano drug-carrying system of equisetin and its derivatives, a preparation method thereof and an application in skin and soft tissue infection MRSA. Background technique [0002] Staphylococcus aureus is an important pathogen, which can cause complicated skin and soft tissue infections, bacteremia, endocarditis and other diseases. The emergence of methicillin-resistant Staphylococcus aureus (MRSA) and its drug resistance have further exacerbated this situation, which prolongs the patient's hospital stay by 66%, and increases the overall cost of treatment and mortality by 54% and 50%, respectively. 64%. MRSA has become one of the three most difficult infectious diseases in the world alongside hepatitis B and AIDS. The rapid spread of MRSA further limits the lifespan of certain antibiotics, necessitating the constant introducti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/4015A61K47/42A61P31/04A61P17/00D04H1/728
CPCA61K9/1075A61K31/4015A61K47/42D04H1/728
Inventor 陈剑鸿石三军罗明和明月李园园
Owner THE THIRD AFFILIATED HOSPITAL INST OF FIELD SURGERY OF PLA ARMY MEDICAL UNIV
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