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188Re-labelled folic acid coupled cis-platinum magnetic albumin compound nano-particle as well as preparation method and application thereof

A technology of albumin nanoparticles and 188re-, which is applied in the field of cisplatin magnetic albumin composite nanoparticles and its preparation, can solve the problems of uneven temperature rise and inability to measure and control temperature, and achieve good stability and anti-tumor pharmacological effects Strong, pure effect

Inactive Publication Date: 2012-10-24
陈道桢 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The latest research believes that if some ferromagnetic substances have the characteristics of Curie temperature (Tc), when the temperature rises to the Curie point, the ferromagnetic substances lose their magnetism and cool down. When the temperature is lower than the Curie point, the ferromagnetic substances It can also achieve automatic temperature control and constant temperature for tumor hyperthermia by restoring the magnetic properties, which overcomes the limitations of traditional hyperthermia inhomogeneous heating and the inability to measure and control temperature. It is of great significance for hyperthermia of deep tumors. As the hot seed of MFH, the magnetosensitive substance has also become a hot research topic in the field of MFH.

Method used

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  • 188Re-labelled folic acid coupled cis-platinum magnetic albumin compound nano-particle as well as preparation method and application thereof
  • 188Re-labelled folic acid coupled cis-platinum magnetic albumin compound nano-particle as well as preparation method and application thereof
  • 188Re-labelled folic acid coupled cis-platinum magnetic albumin compound nano-particle as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: 188 Re-labeled folic acid-coupled cisplatin magnetic albumin composite nanoparticles ( 188 Preparation of Re-folate-CDDP / HAS MNP)

[0036] Add 0.1ml sodium gluconate solution (0.3mol / L), 0.1ml concentrated hydrochloric acid dissolved stannous chloride (10mg / ml), 0.04ml acetic acid buffer solution (pH value 5.0, 0.2mol / L) and 30mg of Folate-ADR-HAS-NP microspheres, shake well and place at room temperature for 1h; then add 188 ReO 4 Eluent 0.1ml, shake well, react at room temperature for 5h, and labeling is completed.

Embodiment 2

[0037] Example 2: 188 Determination of labeling efficiency of Re-labeled folic acid-coupled cisplatin magnetic albumin composite nanoparticles and optimization of labeling conditions

[0038] Thin-layer chromatography was used for analysis. The support was made of GF254 silica gel plate, which was baked in a 56°C oven for half an hour before use. Cut the silica gel plate into strips of about 0.5cm×10cm, mark the origin with a pencil, the origin is about 1cm away from the bottom edge of the test paper, and draw 10 horizontal lines with a pencil at equal distances, a total of 10 grids for later use; take the test tube and make For repeated tube detection, add developing agent, and the developing system is ethanol:ammonia:water (2:1:5v / v). Use a capillary pipette to take the labeled ependoff tube 188 Re-folate-CDDP / HAS MNP, apply the sample at the origin, dry it and run chromatography in the chromatography system. Take out the chromatographic paper and dry it, cut it into 10 ...

Embodiment 3

[0055] Example 3: 188 In Vitro Stability Observation of Re-Folate-ADR / HAS-NP

[0056] Take the composite magnetic nanoparticles marked under Example 1 and wash them twice with distilled water or normal saline, then disperse in 1 mL of calf serum, incubate with shaking at 37°C, at 0, 2, 4, 8, 12, 24, 48 , 72h sampling, and determine the radioactive count. The result is as Figure 5 As shown, it was found that the radiochemical purity was still greater than 80% after being placed at 37° C. for 72 hours. It shows that the marker is stable at 37°C, which can meet the requirements of routine clinical use.

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Abstract

The invention relates to the technical fields of nuclear medicine, oncology and pharmaceutical pharmacy and provides a 188Re-labelled folic acid coupled cis-platinum magnetic albumin compound nano-particle as well as a preparation method and application thereof, wherein the 188Re-labelled folic acid coupled cis-platinum magnetic albumin compound nano-particle has the structure that folic acid active ester is coupled with an amino group on the surface of an albumin nano-particle, 188Re is connected with a hydrosulfide group of cysteine in a protein molecule, and cis-platinum and magnetic particles are packaged in the albumin nano-particle. The invention is mainly applied to the therapy, the diagnosis and the prevention of ovarian cancer tumor and has the advantages that an albumin nano-microsphere is used as a carrier, a folic acid receptor is used as an effect target, and chemotherapy, thermotherapy and nuclide radiotherapy are organically combined together, thereby not only solving the problems of automatic temperature control and constant temperature in tumor thermotherapy, but also solving the problem of directional lethal effect of the chemotherapy and nuclear radiation and satisfying the requirements for three aspects of safety, validity and specificity as far as possible.

Description

technical field [0001] The invention relates to the technical fields of nuclear medicine, oncology and pharmaceutical preparations, in particular to a 188 Re-labeled folic acid-coupled cisplatin magnetic albumin composite nanoparticles and its preparation method and application. Background technique [0002] Ovarian cancer is one of the most common tumors in female reproductive organs, ranking third in incidence after cervical cancer and uterine body cancer. However, the number of deaths due to ovarian cancer ranks first in all types of gynecological tumors, posing a serious threat to women's lives. Although the ovary is small and has complex tissues, it is quite difficult to distinguish its tissue types, benign and malignant. Ovarian cancer is asymptomatic in the early clinical stage. Only 30% of the tumors are found to be confined to the ovary during laparotomy, and most of them have spread to the uterus and bilaterally. 70% of the appendages, omentum and pelvic organs a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/00A61K51/08A61K51/12A61K103/10
Inventor 陈道桢唐秋莎
Owner 陈道桢
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