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Tumor-targeting nanoparticles co-loaded with chemotherapeutic drugs and nucleic acids and preparation method thereof

A chemotherapeutic drug and nanoparticle technology, which is applied in drug combinations, antineoplastic drugs, pharmaceutical formulations, etc., to achieve the effects of easy operation, high biological safety, and simple preparation process

Active Publication Date: 2019-07-26
TIANJIN TUMOR HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there is no report on the use of hyaluronic acid to co-load chemotherapy drugs and nucleic acids to make tumor-targeting nanoparticles

Method used

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  • Tumor-targeting nanoparticles co-loaded with chemotherapeutic drugs and nucleic acids and preparation method thereof
  • Tumor-targeting nanoparticles co-loaded with chemotherapeutic drugs and nucleic acids and preparation method thereof
  • Tumor-targeting nanoparticles co-loaded with chemotherapeutic drugs and nucleic acids and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] (1) Synthesis of polylysine grafted β-cyclodextrin derivatives (PLCD)

[0051] Dissolve 282mg (0.25mmol) of 6-Ald-CD, 57mg (of which the structural unit of lysine is 0.25mmol) of poly-L-lysine hydrobromide in 5mL of acetate buffer solution (0.2M) at pH 4.4 , stirred at room temperature for 1 h, added 62.8 mg (1 mmol) of sodium cyanoborohydride, continued to stir at room temperature for 72 h, added 2M NaOH aqueous solution to adjust the system to neutrality, and then transferred the reaction system to a dialysis bag (molecular weight cut-off of 7000 Da ), dialyzed in ultrapure water for 2 days, and the dialysate was freeze-dried. The resulting white floc product was polylysine-grafted β-cyclodextrin derivative (PLCD), in which the degree of substitution of β-CD was 12.9%.

[0052] The viscosity-average molecular weight of the poly-L-lysine hydrobromide is 15000-30000Da;

[0053] The chemical structure of PLCD was characterized by infrared spectrometer and nuclear magnet...

Embodiment 2

[0067] In vitro drug release experiments

[0068] Take three parts of PDR and HPDR prepared in Example 1, each 1 mL, transfer to a dialysis bag (molecular weight cut-off is 8000 ~ 14000Da), respectively placed in 10 mL of PBS solution with pH 5.0, 6.5 and 7.4, 37 ℃ avoid Light oscillation (100rpm), at different time points (see Figure 8 ) Take out 1.5mL medium for testing, and add an equal volume of fresh dialysis medium; use UV spectrophotometer to detect DOX release (detection wavelength is 480nm). The drug cumulative release rate was calculated according to the following formula: DOX cumulative release rate=(DOX release amount / total amount of DOX input)×100%. DOX release curve see Figure 8 , showing slow drug release characteristics and significant pH sensitivity.

Embodiment 3

[0070] Cellular Uptake Studies

[0071] Replace Control RNA in Example 1 with FAM-RNA, others are the same as Example 1, and the prepared PDR and HPDR are respectively named as PDR FAM and HPDR FAM .

[0072] Examination of PDR by Hepatoma Cell Line MHCC-97H FAM and HPDR FAM The ability and localization of cells; 2 Cultivate in an incubator, the medium is high-sugar DMEM medium containing 10% FBS; when the cells are in the logarithmic growth phase, digest the cells according to 5×10 4 The density of cells / well was seeded in a 12-well plate pre-laid with special glass slides for laser confocal. After 24 hours of culture, free DOX, FAM-RNA, and PDR diluted in serum-free medium were added. FAM and HPDR FAM , so that the final concentration of DOX in the system was 3.3 μg / mL, and the final concentration of FAM-RNA was 1.0 μg / mL; after incubation for 4 hours, the cells were fixed with 4% paraformaldehyde, and the nuclei were stained with DAPI. To observe the fluorescence in ...

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Abstract

The invention discloses tumor-targeting nanoparticles co-loading chemotherapy drug and nucleic acid and a preparation method thereof; the preparation method comprises: (1) preparing polylysine-grafted Beta-cyclodextrin derivative; (2) preparing nanoparticles loading chemotherapy drug; (3) preparing nanoparticles co-loading chemotherapy drug and nucleic acid; (4) preparing tumor-targeting nanoparticles co-loading chemotherapy drug and nucleic acid. The preparation process of the invention is simple and easily operable and saves time and power, and a load material used herein is high in bio-safety and is good in bio-compatibility and biodegradability, zero in toxicity and free of immunogenicity; the tumor-targeting nanoparticles co-loading chemotherapy drug and nucleic acid have typical core-shell structure, are 150-200 nm in particle size, are effective in loading both chemotherapy drug and nucleic acid to cells that highly express CD44 molecules, can inhibit cell proliferation, and have significant in-vivo and in-vitro tumor targeting property.

Description

technical field [0001] The invention belongs to the field of nano-medicines, and in particular relates to a tumor-targeting nano-particle co-carrying chemotherapeutic drugs and nucleic acid and a preparation method thereof. Background technique [0002] The incidence and mortality of malignant tumors are increasing year by year, seriously threatening human health. In recent years, with the continuous improvement of liver surgery techniques, anesthesia techniques, and perioperative management, surgical treatment has become the first choice for the treatment of malignant tumors. However, the vast majority of patients have lost the chance of surgery when they are diagnosed. Chemotherapy is also one of the common strategies to treat malignant tumors. However, due to the heterogeneity of tumors, single chemotherapy often cannot achieve ideal curative effect, and patients tend to develop tolerance to chemotherapy. [0003] In the late 1960s, American scientist Michael Blaese fir...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/40A61K31/704A61K31/4745A61K31/337A61K31/7105A61K31/711A61K48/00A61P35/00
CPCA61K9/5161A61K31/337A61K31/4745A61K31/704A61K31/7105A61K31/711A61K2300/00
Inventor 宋天强熊青青
Owner TIANJIN TUMOR HOSPITAL
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