Preparation method for dual-loaded targeted nano platform of dendrimer based on fluorescent carbon dot modification

A technology of dendritic macromolecules and fluorescent carbon dots, which is applied in the direction of pharmaceutical formulations, preparations for in vivo tests, and medical preparations of non-active ingredients. It can solve problems such as simultaneous connection, achieve reduced inhibitory effects, and good water solubility. and biocompatibility, low-cost effect

Active Publication Date: 2018-11-06
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] At present, the results of domestic and foreign literature searches on dendrimers loaded with anticancer drugs and patents show that the carbon dots connected with the anticancer drug DOX are not connected to

Method used

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  • Preparation method for dual-loaded targeted nano platform of dendrimer based on fluorescent carbon dot modification
  • Preparation method for dual-loaded targeted nano platform of dendrimer based on fluorescent carbon dot modification
  • Preparation method for dual-loaded targeted nano platform of dendrimer based on fluorescent carbon dot modification

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] (1) Add RGD polypeptide solution (6.85 mg, 5 mL DMSO) dropwise to MAL-PEG-COOH (19.83 mg, 5 mL DMSO), stir for 3 days, and then use a dialysis bag with a molecular weight cut-off of 5000 to dialyze the aqueous solution ( 2L / time, 3 times / day), freeze-dry to get RGD-PEG-COOH.

[0051] (2) Add EDC solution (18.21mg, 5mLDMSO) to RGD-PEG-COOH solution (18.33mg, 5mL DMSO), stir at room temperature for 30 minutes, then add NHS solution (9.43mg, 3mL DMSO) and continue stirring for 3 hours to obtain Mixed solution; add the mixed solution dropwise to the fifth generation polyamidoamine dendrimer G5-NH 2 solution (38.34mg, 10mL DMSO), the stirring reaction time was 3 days, and then the aqueous solution was dialyzed (2L / time, 3 times / day) using a dialysis bag with a molecular weight cut-off MWCO of 5000, and freeze-dried to obtain G5-PEG- RGD.

[0052] (3) Add CDI solution (25.23mg, 10mL DMSO) to TPGS solution (10.10mg, 4mL DMSO), stir at room temperature for 6 hours, then add G...

Embodiment 2

[0057] Take the RGD-PEG-COOH prepared in Example 1, G5-PEG-RGD and G5-RGD-TPGS were dissolved in D 2 In O, use Bruker400MHz nuclear magnetic resonance instrument to carry out hydrogen spectrum test. see figure 2 a, In the H NMR spectrum of RGD-PEG-COOH, 3.6ppm is the characteristic proton peak of MAL-PEG-COOH, and 7.15-7.25 is the characteristic proton peak of the benzene ring on RGD. According to the ratio of their integral areas, calculate It is found that 0.89 RGD molecules are linked to each PEG (the molar ratio of the feed is MAL-PEG-COOH:RGD=1:1). see figure 2 b, 2.0-3.6ppm is dendrimer G5.NH 2 The methylene proton peaks, according to the ratio of their integral areas, calculate each G5.NH 2 3.86 PEG-RGD molecules are linked on the above (the molar ratio of the feed is G5.NH2:PEG-RGD=1:5). see figure 2 c, 0.7ppm is the methyl proton peak of TPGS, according to the ratio of their integrated areas, calculates that 9.7 TPGS molecules are linked on each G5-RGD molecu...

Embodiment 3

[0059] Dissolve the (CDs-DOX)@G5-RGD-TPGS prepared in Example 1 with pH=7.4 and pH=5.5 buffers respectively to a solution with a concentration of 1mg / mL, take 1mL into a dialysis bag for fixation, and place Place in a container containing 9mL of buffer solution of different pH and shake in a shaker at 37°C. Samples were taken at different time points. Take 1mL of the liquid outside the dialysis bag each time, measure its absorbance at 480nm, and then add 1mL of the corresponding buffer solution to the outside of the dialysis bag. This method was used to obtain the release curves of DOX released from (CDs-DOX)@G5-RGD-TPGS under different pH conditions in vitro. see Figure 4 B, In 70 hours, the release amount of DOX was 48% in a weakly acidic environment (pH=5.5), which was greater than 29.5% in a physiological environment (pH=7.4). It shows that this drug-loading system has a certain pH responsiveness, and the release rate in the weakly acidic environment similar to tumor t...

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Abstract

The invention relates to a preparation method for a dual-loaded targeted nano platform of dendrimer based on fluorescent carbon dot modification. The method includes carbon spot preparation, preparation of a drug sustained release system with fluorescent carbon spots loaded with doxorubicin, RGD-PEG-COOH preparation, RGD-targeted functional dendrimer G5-PEG-RGD preparation, G5-RGD-TPGS preparationand CDs/DOX@G5-RGD-TPGS preparation. The obtained (CDs/DOX)@G5-RGD-TPGS dual-loaded nanoparticles have good water solubility and biocompatibility, are targeted to tumor cells expressed by the integrin AlphavBeta3 receptor, have an obvious inhibitory effect on the tumor cells, can reduce the level of intracellular ATP and hinder the drug pumping, can be used for fluorescence imaging of cancer cells and have the diagnosis and treatment integration performance.

Description

technical field [0001] The invention belongs to the field of preparation of functional hybrid nanomaterials, in particular to a preparation method of a double drug-loaded targeting nanometer platform based on dendrimer modified by fluorescent carbon dots. Background technique [0002] Fluorescence imaging technology has the advantages of high temporal / spatial resolution, high soft tissue contrast, rich information and low price. However, the preparation methods of fluorescent molecules such as organic dyes or semiconductor quantum dots are cumbersome, expensive, environmentally unfriendly and prone to photobleaching. Therefore, the development of a new type of environmentally friendly fluorescent molecules is one of the development trends of fluorescence imaging. [0003] Carbon dots (carbon dots) is a kind of spherical nanomaterials with fluorescence properties, the size is below 10nm, which can emit bright fluorescence (Miao, P., et al., Nanoscale, 2015.7 (5): p.1586-1595...

Claims

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Application Information

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IPC IPC(8): A61K47/60A61K31/704A61P35/00A61K49/00
CPCA61K31/704A61K49/0019A61K47/60A61P35/00
Inventor 史向阳李丹范钰
Owner DONGHUA UNIV
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