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Salinomycin-loaded micelles, preparation method and application thereof

A technology containing salinomycin and salinomycin sodium, applied in the field of medicine, can solve the problems of systemic toxicity, no liver cancer treatment, and difficulty in eradicating liver cancer recurrence, and achieves the effect of broad application prospects.

Inactive Publication Date: 2017-01-11
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these chemotherapeutic drugs not only have serious systemic toxicity, but also usually have no obvious disease-modifying or life-prolonging effect
There is a common problem in the current treatment methods: the first-line drugs used in the treatment of liver cancer in these therapies are all aimed at differentiated tumor cells, which can kill such cells in a short period of time, making the tumor volume decrease or even disappear, but It is difficult to eradicate the recurrence of liver cancer, and the root cause of liver cancer has not been treated
[0010] At present, there is no literature report on using DSPE-PEG2000-CRGDK copolymer as a carrier to load salinomycin into micelles for targeted drug delivery on liver cancer cells and stem cells

Method used

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  • Salinomycin-loaded micelles, preparation method and application thereof
  • Salinomycin-loaded micelles, preparation method and application thereof
  • Salinomycin-loaded micelles, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Embodiment 1: the synthesis of the block copolymer of DSPE-PEG2000-CRGDK

[0076] Such as figure 1 As shown in A, accurately weigh 0.3mg CRGDK and 1.5mg DSPE-PEG2000-MAL and dissolve them in 2ml 50mM HEPES buffer solution (pH 6.5), and magnetically stir at room temperature for 48h. - Maleimide group binding in PEG2000-MAL. After the reaction, the reaction solution was put into a dialysis bag (Spectra / Por, MWCO1000), and dialyzed in deionized water for 24 hours, wherein the dialysate was changed every 12 hours.

[0077] After dialysis, the solution in the bag was freeze-dried for use.

[0078] The result is as figure 1 As shown in B, the relative molecular weight of DSPE-PEG2000 is concentrated in 2800-3400, while figure 1 C DSPE-PEG2000-CRGDK has a peak at 3500-4000, and the increased molecular weight value is consistent with the molecular weight of CRGDK at 700. The results show that CRGDK is successfully connected to DSPE-PEG2000.

Embodiment 2

[0079] Embodiment 2: the preparation of salinomycin sodium micelle

[0080] Such as figure 2 As indicated, dissolve 1mg DSPE-PEG2000-CRGDK and 4mg DSPE-PEG2000 in 3ml chloroform, and dissolve another 0.5mg salinomycin sodium in 1ml methanol, mix the above two solutions, and evaporate under reduced pressure at 35°C for 4h The organic solvent is removed to form a dry film. Add 2 mL of pH 7.4 phosphate buffer to the bottle and fill it with nitrogen gas, and hydrate for 30 min. Unencapsulated salinomycin sodium was removed by passing through a 50 nm polycarbonate membrane.

[0081] The size of the micelles prepared by thin film dispersion method is at 13nm ( image 3 A), the zeta potential is maintained at around -13mV ( image 3 B), transmission electron microscope ( image 3C) shows that the DSPE-PEG2000-CRGDK mixed micelles prepared by the present invention are spherical and have a typical core-shell structure. This experiment shows that the DSPE-PEG2000-CRGDK self-assem...

Embodiment 3

[0082] Embodiment 3: Optimization of the preparation process of salinomycin micelles

[0083] (1) Screening of carrier total amount and salinomycin sodium mass ratio

[0084] Dissolve (0.5, 1, 1.5) mg DSPE-PEG2000-CRGDK and (2,4,6) mg DSPE-PEG2000 in 3ml chloroform respectively, and dissolve another 0.5mg salinomycin in 1ml methanol, (i.e. the total amount of carrier The mass ratio to salinomycin sodium is 1:5, 1:10, and 1:15 respectively) Mix the above two solutions, and remove the organic solvent by rotary evaporation under reduced pressure at 35°C for 4 hours to form a dry film. Add 2 mL of pH 7.4 phosphate buffer to the bottle and fill it with nitrogen gas, and hydrate for 30 min. Unencapsulated salinomycin sodium was removed by passing through a 50 nm polycarbonate membrane. The results showed that when the mass ratio was 1:10, the encapsulation efficiency of micelles was the highest, see Table 1 for details.

[0085] Table 1: Effects of the ratio of the total mass of ...

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Abstract

The invention discloses a salinomycin-loaded micelle as well as a preparation method and application thereof, belonging to the technical field of medicines. The salinomycin-loaded micelle disclosed by the invention is a small-granularity micelle which is high in targeting and infiltration capacity; in the salinomycin-loaded micelle, sodium salinomycin is loaded on DSPE-PEG2000-CRGDK copolymer which serves as a carrier. Furthermore, the invention discloses a preparation method of the micelle as well as application of the micelle in preparation of a medicine for treating liver cancer. The salinomycin-loaded micelle disclosed by the invention can simultaneously differentiate liver cancer cells and liver cancer stem cells in a targeting manner. The invention provides a new strategy for treating liver cancer; based on the combination of the advantages of the micelle carrier and high-infiltration targeting peptide CRGDK, an effect of targeting the liver cancer cells and liver cancer stem cells is achieved, so as to fundamentally treat the liver cancer; and the micelle has a broad application prospect.

Description

[0001] Technical field: [0002] The invention belongs to the technical field of medicine, and in particular relates to a pharmaceutical preparation of salinomycin-loaded micelles combined with membrane-penetrating peptide CRGDK targeting liver cancer stem cells, as well as its preparation and application. [0003] Background technique: [0004] Liver cancer is one of the common malignant tumors in my country. Because of its high degree of malignancy, rapid disease progression, and no obvious symptoms in the early stage, the liver has been severely damaged when it is diagnosed. Therefore, it is difficult to treat, has poor curative effect, and has a high mortality rate. The king of cancer". Therefore, the prevention and treatment of liver cancer has become an important task of medical research in our country. [0005] Since the liver has been severely damaged when liver cancer occurs, the specific treatment options are greatly restricted. Although biological therapy has made g...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K31/7048A61K47/42A61P35/00
Inventor 钟延强毛骁丽张翮鲁莹邹豪陈琰俞媛高静刘俊杰孙治国解方圆巩志荣何文婷张思悦陈大中王美平
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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