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Target PEG (Polyethylene Glycol) modified gold nanorod and AlpcS4 coupled combination as well as preparation, application and antitumor composition thereof

A technology of gold nanorods and conjugates, which is applied in the field of anti-tumor drug research, can solve the problems of limited photodynamic effect, low drug delivery efficiency, limited tumor tissue selectivity and enrichment ability, etc., to reduce toxic and side effects and improve gastric cancer. Therapeutic effect, the effect of circumventing multidrug resistance

Active Publication Date: 2017-12-15
XI AN JIAOTONG UNIV
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Problems solved by technology

[0008] The object of the present invention is to provide a combination of PEG-modified gold nanorods and photosensitizer AlpcS4, with the help of the passive targeting ability of gold nanorods, improve the drug delivery efficiency of AlpcS4, and solve the problem of AlpcS4 drug delivery efficiency is low, photosensitive Issues of limited kinetic effect, limited selectivity and enrichment capacity for tumor tissue
[0009] The purpose of the present invention is also to provide a preparation method and application of a conjugated target PEG-modified gold nanorods coupled with photosensitizer AlpcS4, further making the conjugates more specific to the tumor site, and further solving the problem of tumor tissue selectivity and The problem of limited enrichment ability, a greater degree of selective killing of tumor cells

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  • Target PEG (Polyethylene Glycol) modified gold nanorod and AlpcS4 coupled combination as well as preparation, application and antitumor composition thereof
  • Target PEG (Polyethylene Glycol) modified gold nanorod and AlpcS4 coupled combination as well as preparation, application and antitumor composition thereof
  • Target PEG (Polyethylene Glycol) modified gold nanorod and AlpcS4 coupled combination as well as preparation, application and antitumor composition thereof

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Embodiment Construction

[0057] The present invention will be further described in detail below in conjunction with specific embodiments, which are explanations of the present invention rather than limitations.

[0058] 1. Preparation and characterization of gold nanorods

[0059] The present invention adopts NaBH 4 As the reducing agent, CTAB is the gold seed growth method of the stabilizer to prepare gold nanorods. The specific synthesis is as follows:

[0060] Preparation of gold seeds: prepare 7.5ml 100mM CTAB aqueous solution, mix with 250uL 10mM HAuCl 4 The aqueous solution is mixed and stirred, and 600uL 10mM NaBH is added during the stirring process 4 Stir for 2 minutes, stand at 27°C for 2 hours; preparation of growth solution: prepare 10ml of 100mM CTAB aqueous solution, add 0.8mL of 10mM HAuCl to it 4 aqueous solution, followed by sequential addition of 425uL 10mMAgNO 3 Aqueous solution, 90uL of 100mM vitamin C solution for anti-oxidation, 100uL of 1% HCl; add 105uL of seed solution int...

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Abstract

The invention provides a target PEG (Polyethylene Glycol) modified gold nanorod and AlpcS4 coupled combination, preparation and application thereof, and an antitumor composition. The combination comprises AlPcS4 and PEG modified gold nanorods, wherein the PEG modified gold nanorods are gold nanorods modified by HS-PEG-COOH; carboxyl of HS-PEG-COOH is connected with polypeptides or target oligopeptides through amido bonds; AlPcS4 is adsorbed to the surfaces of the gold nanorods through electrostatic adsorption; and the surface plasmon resonance peak of the PEG modified gold nanorods is 750-850 nm. By adopting the combination, the medicine transmission efficiency of AlPcS4 can be improved by virtue of passive targeting capability of the gold nanorods or active targeting capability of target molecules, and the problems that an AlpcS4 medicine is low in transmission efficiency, limited in photodynamic effect and limited in tumor tissue selectivity and enrichment capacity are solved.

Description

technical field [0001] The present invention relates to the field of anti-tumor drug research, in particular to a combination of targeted PEG-modified gold nanorods coupled with a photosensitizer AlpcS4, a preparation method and application thereof, and an anti-tumor composition based on the combination. Background technique [0002] Malignant tumors are common and serious diseases that seriously endanger human life and health. Over the years, the proportion of deaths due to it remains high. Gastric cancer, in particular, ranks second among malignant tumors, with a new incidence rate of up to 400,000 people per year and a death rate of up to 300,000 people, ranking first in the world. However, its incidence rate in western countries is relatively low. Ji Jiafu pointed out that nearly half of the world's new gastric cancer cases occur in China every year, accounting for as much as 47%. This makes gastric cancer one of the major diseases that must be overcome independently in...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K47/69A61K47/60A61K47/64A61P35/00A61K31/122A61K31/475A61K31/407A61K33/24
CPCA61K31/122A61K31/407A61K31/475A61K33/24A61K41/0076A61K2300/00
Inventor 辛静张镇西姚翠萍王斯佳王晶张璐薇付磊王兵
Owner XI AN JIAOTONG UNIV
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