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A kind of tadalafil supramolecular nanoparticle and its preparation method and application

A nanoparticle and tadalafil technology, which is applied in the field of chemical drugs and biological applications, can solve difficult problems such as tumor metastasis, and achieve the effect of broad application prospects, high affinity, and high drug loading capacity

Active Publication Date: 2021-12-24
SOUTHWEST UNIV
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

However, 90% of the deaths caused by cancer are related to tumor metastasis, and these traditional therapies are difficult to overcome the problem of tumor metastasis

Method used

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  • A kind of tadalafil supramolecular nanoparticle and its preparation method and application
  • A kind of tadalafil supramolecular nanoparticle and its preparation method and application
  • A kind of tadalafil supramolecular nanoparticle and its preparation method and application

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Embodiment 1

[0028] Example 1 Preparation of Tadalafil Supramolecular Nanoparticles

[0029] like figure 1 The synthesis schematic shown in the preparation of GSH-sensitive tadalafil supramolecular nanoparticles includes the following steps:

[0030] (1) Dissolve 4 mg of indocyanine green ICG solid powder in 5 mL of a mixed solvent of methanol and water at a room temperature of 25 °C to obtain an ICG solution. The volume ratio of methanol to water is 2:1, and then add to it Add 5 mL of Fe 3+ (64.5 μM, FeCl 3 ) solution, and stirred for 4h in the dark to obtain Fe containing 3+ ICG solution;

[0031] (2) Dissolve 8 mg of tadalafil TAD solid powder in 2 mL of chloroform solution, and sonicate for 5 minutes to obtain a TAD solution;

[0032] (3) Under ultrasonic conditions, add the TAD solution obtained in step (2) dropwise to the Fe-containing 3+ In the ICG solution, continue to sonicate for 5 minutes, and then let it stand for 5 minutes to obtain a mixed solution;

[0033] (4) Use a ...

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Abstract

The invention specifically relates to a tadalafil supramolecular nanoparticle and a preparation method and application thereof. The specific preparation methods include: (1) using Fe 3+ It binds with the phototherapy drug indocyanine green ICG through coordination interaction; (2) the immunosuppressant tadalafil TAD binds with ICG / Fe 3+ Self-assembly of Fe by π-π stacking interactions between benzene rings 3+ / ICG@TAD nanoparticles. The preparation method is simple and feasible, the obtained nanoparticles have high micellar stability, high drug loading, and under the GSH reduction conditions with high tumor microenvironment, Fe 3+ When reduced, the nanoparticles are decomposed, which in turn selectively releases the drug. This strategy effectively solves the disadvantages of hydrophobic drug molecules in drug delivery systems, such as poor water solubility and large toxic and side effects. The synergistic effect of immunosuppressive drugs and phototherapy drugs shows enhanced tumor suppressive ability and has broad application prospects in synergistic immunotherapy.

Description

technical field [0001] The invention relates to the field of chemical medicine and biological application, in particular to a tadalafil supramolecular nanoparticle and a preparation method and application thereof. Background technique [0002] Cancer, as a disease with a high mortality rate, is a major health problem facing human beings. At present, clinical cancer treatment methods mainly include surgery, radiotherapy and chemotherapy, and these treatments have a certain degree of curative ability for some primary tumors. However, 90% of cancer-related deaths are related to tumor metastasis, and these traditional therapies are difficult to overcome the problem of tumor metastasis. By regulating the autoimmune system and enhancing the immune response, immunotherapy helps to improve the survival rate of patients and prevent tumor recurrence and metastasis, which has brought revolutionary progress in the field of cancer treatment. Immune checkpoint blockade can promote the p...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K41/00A61K31/4985A61P35/00
CPCA61K9/51A61K41/0057A61K31/4985A61P35/00A61K2300/00
Inventor 许志刚梁梦云张天马宪彬康跃军
Owner SOUTHWEST UNIV
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