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Preparation and application of near-infrared light activated drug self-delivery nano preparation

A nano-preparation and near-infrared light technology, which is applied in the direction of drug combinations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of high drug toxicity, difficulty in skin absorption, and difficulty in administration. Achieve the effects of increasing accumulation and deep penetration, improving difficult absorption, and prolonging blood circulation time

Pending Publication Date: 2022-04-01
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] At the same time, phototherapy is also widely used in other fields, such as wound infection and other skin diseases, but the development of related photosensitizers is only the second generation of chlorin drugs. The problem of potential excessive toxicity of drugs, and how to better apply phototherapy drugs to superficial skin diseases and the field of medical aesthetics still exist

Method used

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  • Preparation and application of near-infrared light activated drug self-delivery nano preparation
  • Preparation and application of near-infrared light activated drug self-delivery nano preparation
  • Preparation and application of near-infrared light activated drug self-delivery nano preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1: Preparation of near-infrared light-activated drug self-delivery nano-formulations

[0043]Dissolve indocyanine green in pure water, dissolve imiquimod in DMSO, and add 1:1 to the prepared pure water successively to obtain a mixed solution of indocyanine green and imiquimod; mix the obtained The solution was stirred for 10-100 minutes, and 10 μM dopamine hydrochloride solution was added, and the stirring was continued for 10-100 minutes to obtain the unpurified nano-preparation; the unpurified nano-preparation was dialyzed in a dialysis bag with a molecular weight cut-off of 1000D for 24 hours, purified and concentrated Afterwards, the above-mentioned near-infrared light-activated drug self-delivery nano-preparation was obtained and stored at -20°C.

Embodiment 2

[0044] Example 2: Detection of properties of near-infrared light-activated drug self-delivery nano-preparations

[0045] The properties of the near-infrared light-activated drug self-delivery nano-preparation obtained in Example 1 were tested, in which transmission electron microscope detection and dynamic light scattering detection were respectively carried out.

[0046] Among them, through figure 1 It can be seen from the transmission electron microscope examination shown that the near-infrared light-activated drug self-delivery nano-preparation obtained in Example 1 is in a good dispersion state in water, and is a spherical nano-preparation with uniform size.

[0047] pass figure 2 From the results of dynamic light scattering shown, it can be seen that the particle size of the near-infrared light-activated drug self-delivery nano-preparation obtained in Example 1 is mainly concentrated at about 70-80nm, which is the best retention and uptake range for tumor tissues report...

Embodiment 3

[0048] Example 3: Stability testing of near-infrared light-activated drug self-delivery nano-preparations

[0049] Stability testing was performed on the near-infrared light-activated drug self-delivery nano-preparation obtained in Example 1, in which the change of solution absorbance under near-infrared laser irradiation and the imaging test of the solution sample after repeated lyophilization and dissolution were respectively carried out.

[0050] The change of the absorbance of the solution under near-infrared laser irradiation is as follows: image 3 As shown, the results show that compared with the small molecule indocyanine green, the absorbance of the nano-preparation does not decrease significantly under laser irradiation, indicating that the photostability of the nano-preparation is good, and subsequent experiments can be carried out. At the same time, the photos of repeated dissolution after lyophilization are as follows: Figure 4 As shown, the solution did not det...

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Abstract

The invention relates to a preparation method of a drug self-delivery nano preparation activated by near-infrared light and application of the drug self-delivery nano preparation in tumor photoimmunotherapy, and belongs to the field of pharmaceutical preparations. The near-infrared light activated drug self-delivery nano preparation provided by the invention is based on two small molecule drugs approved by FDA and a dopamine shell layer, self-assembly of the novel nano preparation is realized without assistance of a delivery carrier, and a tumor vaccine capable of being intravenously injected is obtained. The photosensitizer provided by the invention can improve the defects of difficult administration and large toxicity of the existing clinical photosensitizer, improves the accumulation and deep penetration of the drug at the tumor site, and can effectively realize tumor photoimmunotherapy under the irradiation of near-infrared light. The method has high application value in treatment of malignant tumors, bacterial infection and superficial skin diseases. The preparation method of the nano preparation provided by the invention is rapid and simple, all components in the nano preparation are approved by FDA, the safety is good, large-scale standardized production is realized, and huge potential is provided for industrial production and clinical transformation of the technology.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to the preparation and application of a near-infrared light-activated drug self-delivery nano-preparation. Background technique [0002] Tumor immunotherapy is to inhibit tumor growth and metastasis by activating and enhancing the body's own immune system to generate anti-tumor immunity. It has developed rapidly in recent years and is considered to be a very promising tumor treatment strategy. At present, a variety of immune checkpoint inhibitor drugs have been approved by the FDA for the treatment of melanoma and non-small cell lung cancer. However, there are still problems such as low immune response rate and immunosuppression of the tumor microenvironment, which make the effect of immunotherapy far lower than expected, and the development of tumor vaccines still faces many problems. [0003] Immunogenic cell death of tumor cells is a special form of apoptosis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/34A61K41/00A61K31/4745A61P17/00A61P17/06A61P17/10A61P17/12A61P31/04A61P31/12A61P35/00
Inventor 赵炜王朔孟萌白月苹
Owner NANKAI UNIV
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