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A hypoxia responsive liposome preparation and its preparation method and application

A liposome preparation and liposome technology, applied in the field of biomedicine, can solve the problems of limited killing ability of cancer cells, damage to the structure of blood vessels, consumption of large oxygen, etc. Effect

Active Publication Date: 2019-04-26
SUZHOU INNOVATIVE BIOMATERIALS & PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, a large number of studies have shown that photodynamic therapy only has a good killing effect on cancer cells in areas with high oxygen content in tumor tissues, and has limited killing ability on cancer cells in hypoxic areas.
At the same time, due to the consumption of a large amount of oxygen and the destruction of vascular structures during photodynamic therapy, the tumor tissue after photodynamic therapy will become more hypoxic, and eventually the expected therapeutic effect cannot be achieved.

Method used

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  • A hypoxia responsive liposome preparation and its preparation method and application
  • A hypoxia responsive liposome preparation and its preparation method and application
  • A hypoxia responsive liposome preparation and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1, the preparation of liposome-AQ4N-chlorin e6 preparation

[0038] After weighing DPPC, DSPE-PEG, CH, and Ce6 according to the molar ratio of 6:0.5:4:0.5, they were dissolved in chloroform solution, and the chloroform solution was blown dry with nitrogen. Weigh AQ4N and dissolve it in phosphate buffer to prepare a 10 mg / mL AQ4N solution and add the prepared solution into liposome-chlorin e6, stir in a water bath at 50°C for 30 minutes, and place the prepared liposome - AQ4N- Chlorin e6 formulation extruded film.

Embodiment 2

[0039] Embodiment 2, the property detection of liposome-AQ4N-chlorin e6 preparation

[0040] The liposome-AQ4N-chlorin e6 preparation prepared in Example 1 was qualitatively detected, and transmission electron microscope detection, dynamic light scattering, and ultraviolet absorption were respectively carried out.

[0041] Among them, the results of transmission electron microscope detection are as follows: figure 1 As shown, the results show that the liposome-AQ4N-chlorin e6 preparation prepared in Example 1 is distributed in a monodisperse state in water, indicating that the liposome-AQ4N-chlorin e6 preparation prepared by the present invention Uniform particle size, well dispersed in water.

[0042] The results of dynamic light scattering were as follows: figure 2 As shown, the results show that the particle size of the liposome-AQ4N-chlorin e6 preparation prepared in Example 1 is mainly concentrated at about 100nm in water.

[0043] The results of the UV absorption tes...

Embodiment 3

[0044] Embodiment 3, the photodynamic activity detection of liposome-AQ4N-chlorin e6 preparation

[0045] Prepare the aqueous solution of liposome-AQ4N-chlorin e6 preparation, irradiate with 660nm laser, detect the singlet oxygen content, set up liposome-AQ4N-chlorin e6 aqueous solution group, liposome-chlorin e6 Phene e6 aqueous solution group, phosphate buffer saline group. see results Figure 4 .

[0046] Figure 4 The results showed that the solutions containing the photosensitive molecule chlorin e6 all produced singlet oxygen after laser irradiation, and could be used as photodynamic therapy agents.

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Abstract

The invention relates to the technical field of biomedicines and relates to a hypoxia responsive liposome preparation, and preparation and applications thereof. In particular, the invention relates to hypoxia responsive liposome-AQ4N-dihydroporphin e6 and preparation and application thereof, and especially, application thereof in enhancement of killing cells in tumor hypoxia zones in photodynamics therapy. The liposome preparation is composed of a liposome, AQ4N and dihydroporphin e6, has uniform particle size and is excellent in dispersion in water. The particle size of the liposome preparation is mainly about 100 nm in water. The liposome preparation can carry photosensitive molecules and dimethyldiguanide and is an ideal medicine carrier, and also has excellent in-vivo pharmacokinetics behavior. A test proves that the liposome-AQ4N-dihydroporphin e6 preparation is very-highly enriched at tumor parts, so that after the photodynamics therapy, the preparation can cause a more serious hypoxia status in the tumor zone, thereby improving the killing effect on the hypoxia cells of the AQ4N and obtaining excellent synergistic therapy effects on tumor.

Description

technical field [0001] The present invention relates to the technical field of biomedicine, and relates to a hypoxia-responsive liposome preparation and its preparation and application, in particular to liposome-AQ4N-chlorin e6 and its preparation and application, especially its ability to enhance light Application of dynamic therapy to cell killing in tumor hypoxic zone. Background technique [0002] Tumor refers to the neogrowth formed by the proliferation of local tissue cells in the body under the action of various tumorigenic factors, because this neogrowth is mostly in the form of space-occupying blocky protrusions, also known as neoplasm (neoplasm) . According to the cell characteristics of new organisms and the degree of harm to the body, tumors are divided into two categories: benign tumors and malignant tumors, and cancer is the general term for malignant tumors. Compared with benign tumors, malignant tumors grow faster and show invasive growth, are prone to blee...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K41/00A61K31/14A61P35/00
CPCA61K9/127A61K31/14A61K41/0071A61K2300/00
Inventor 刘庄冯良珠
Owner SUZHOU INNOVATIVE BIOMATERIALS & PHARM CO LTD
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