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USPIO-PLA-RGD compound, preparation method and application thereof

A technology of complex and hydrated particle size, which is applied in the field of USPIO-PLA-RGD complex and its preparation, can solve the problem of unsatisfactory molecular imaging effect, and achieve strong affinity, obvious biological effect, good biocompatibility and stability sexual effect

Inactive Publication Date: 2009-12-02
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The results show that the RGD peptide-modified USPIO nanomagnetic probe has a good effect on targeting the integrin αvβ3 receptor of neovascular endothelial cells in vitro, but the molecular imaging effect in vivo is not ideal

Method used

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  • USPIO-PLA-RGD compound, preparation method and application thereof
  • USPIO-PLA-RGD compound, preparation method and application thereof
  • USPIO-PLA-RGD compound, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Preparation of USPIO-PLA-RGD complex

[0030] 1. Synthesis of PLA-USPIO

[0031] 730 mg FeCl 3 .6H 2 O and 300 mg FeCl 2 .4H 2 O dissolved in 20ml of a mixed solution of deionized water and ethanol containing 20% ​​ethanol, Fe 2+ with Fe 3+ The molar ratio is about 1:2. Dissolve 2g of polylactic acid in the above solution, and if necessary, use ultrasound to fully and uniformly disperse the components in the solution system. Under nitrogen protection, add 5M NaOH or 28% NH dropwise 3 .H 2 O, bring the pH value to 10, and stir the reaction vigorously for half an hour. The reaction solution was taken out and aged in a water bath at 80° C. for 2 hours to promote crystal maturity. Wash with deionized water, centrifuge at 10,000 rpm for 5 times for 10 minutes to obtain magnetic nanoparticles, and adjust the concentration of Fe ions to 5 mg / ml.

[0032] 2. Coupling of RGD and PLA-USPIO

[0033] Take 100 μl of PLA-USPIO with an Fe ion concentration of 5 ...

Embodiment 2

[0034] Example 2: In vitro characterization of the RGD-PLA-USPIO complex

[0035] 1) Transmission electron microscope: The transmission electron microscope picture is as follows figure 1 as shown, figure 1 It was shown that the particle size of the core USPIO of the USPIO-PLA-RGD complex was around 3-5nm.

[0036] 2) Dynamic light scattering: the PLA-USPIO aqueous solution and the RGD-PLA-USPIO aqueous solution prepared in Example 1 were respectively placed in a particle size analyzer, and the dynamic light scattering spectra were as follows: figure 2 and image 3 As shown, the results show that the hydrated particle size of PLA-USPIO is about 62nm, and the hydrated particle size of RGD-PLA-USPIO is about 95nm.

[0037] 3) FT-IR: RGD-PLA-USPIO was lyophilized and the solid was taken for FT-IR, and carboxyl peaks could be observed on the spectral line.

[0038] 4) In vitro experiment of RGD-PLA-USPIO

[0039] Human umbilical vein endothelial cells HUVECs (gifted by the Sc...

Embodiment 3

[0040] Example 3: Experiments on RGD-PLA-USPIO tumor-bearing animals

[0041] 1) Preparation of rabbit VX2 tumor model

[0042] Purebred New Zealand white rabbits, aged 2-3 months, male or female, weighing 1.6-1.8kg. After successful intramuscular injection of a mixed solution of midazolam injection (5mg / kg) and ketamine hydrochloride injection (25mg / kg) for anesthesia, routine depilation and disinfection of the outer skin of the proximal part of one side of the thigh, and 0.1ml of VX2 tumor tissue suspension Inject into the vastus lateralis muscle of the thigh and form a mold in about 2 weeks. The tumor was a sub-round solid mass with a clear capsule and homogeneous internal signals.

[0043] 2) MR imaging of experimental animals

[0044] New Zealand big-eared white rabbits inoculated with VX in the hind limbs 2 Tumors, ready for use in about two weeks. Anesthesia was performed before drug injection, and a catheter was placed in the marginal ear vein, and a plain scan wa...

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Abstract

The invention discloses a USPIO-PLA-RGD compound, a preparation method and application thereof. The USPIO-PLA-RGD compound uses USPIO as a core, is coated by PLA outside, and is labeled as PLA-USPIO; and the USPIO-PLA-GRD compound obtained through covalently coupling carboxyl of a functional group exposed on the surface of PLA and amidogen of RGD peptide has a hydrated grain diameter of between 90 and 105 nm. The USPIO-PLA-RGD compound can be applied as magnetic resonance tumor angiogenesis targeting contrast agent. The invention realizes targeting developing by the characteristics of high affinity of an alpha v beta3 integrin receptor and ligand RGD peptide thereof, and the combination has the characteristics of high specificity, selectivity, saturation and affinity, clear biological effect and the like. The concentration of a medicament in a partial focus can be increased, and toxic and side effects can be reduced by using the ligand RGD peptide as a vector of USPIO through the mediation effect of the receptor, so that the aim of development of a targeting tumor angiogenesis living body is realized.

Description

1. Technical field [0001] The invention belongs to the technical field of medical detection reagents, and relates to a USPIO-PLA-RGD complex and its preparation method and application, especially its application as a contrast agent capable of specifically imaging neovascularization of tumors in magnetic resonance imaging. 2. Background technology [0002] Tumor growth, invasion, metastasis, and prognosis are closely related to microangiogenesis. The traditional "gold standard" for quantitative evaluation of tumor angiogenesis - tumor MVD (Mean Vascular Density) counting is not an effective method due to its shortcomings such as invasiveness, dependence on accurate sampling, and inability to perform functional evaluation of tumor angiogenesis activity. Ideal means of inspection. Therefore, finding a non-invasive, accurate, reproducible imaging method in vivo that can obtain direct quantitative information on tumor microangiogenesis has always been one of the important topics...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/06
Inventor 张敏鸣张景峰武新英毛晖林冰影谭延斌
Owner ZHEJIANG UNIV
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