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Preparation method for RGD-targeted porphyrin polymer nanomicelle

A porphyrin polymer and nanomicelle technology is applied in the field of polymer nanomicelle preparation, which can solve the problems of low target cell selectivity and low drug entrapment rate.

Active Publication Date: 2015-01-14
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Aiming at the above prior art, the present invention provides a method for preparing RGD-targeted porphyrin polymer nanomicelles. The RGD-targeted porphyrin polymer nanomicelles obtained in the present invention have their own photosensitivity activity. By further loading chemical drugs To realize the curative effect of chemotherapy, it solves the technical problem of low drug embedding rate of the drug co-delivery carrier; in addition, the drug carrier is delivered into the tumor cell through the targeting effect of RGD, which solves the problem of low selectivity of the non-targeted drug delivery carrier to the target cell. technical problem

Method used

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  • Preparation method for RGD-targeted porphyrin polymer nanomicelle
  • Preparation method for RGD-targeted porphyrin polymer nanomicelle
  • Preparation method for RGD-targeted porphyrin polymer nanomicelle

Examples

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Embodiment 1

[0020] In this example 1, the selected carboxyl-terminated porphyrin-amphiphilic block copolymer is carboxyl-terminated 5-(3-hydroxyphenyl)-10,15,20-triphenylporphyrin / Polyethylene lactide / polyethylene glycol block copolymer, the selected hydrophobic drug is paclitaxel, and the steps for preparing RGD-targeted paclitaxel porphyrin polymer nanomicelle are as follows:

[0021] 1) Carboxyl-terminated 5-(3-hydroxyphenyl)-10,15,20-triphenylporphyrin / polyethylene lactide / polyethylene glycol block copolymer with a molar ratio of 1:25 The RGD peptide is mixed and added to the carboxyl-terminated 5-(3-hydroxyphenyl)-10,15,20-triphenylporphyrin / polyethylene lactide / polyethylene glycol block copolymer molecule The carboxyl-terminal equivalent carbodiimide cross-linking agent was reacted at 25°C for 45 hours to connect the RGD peptide to the carboxyl-terminated 5-(3-hydroxyphenyl)-10,15 , 20-triphenylporphyrin / polyethylene lactide / polyethylene glycol block copolymer;

[0022] 2) Dissol...

Embodiment 2

[0027] In Example 2, the selected carboxyl-terminated porphyrin-amphiphilic block copolymer is carboxyl-terminated 5,15-bis(3-hydroxyphenyl)-10,20-diphenylporphyrin / polyethylene lactide / polyethylene glycol block copolymer, the selected hydrophobic drug is docetaxel, and the steps for preparing RGD-targeted docetaxel porphyrin polymer nanomicelle are as follows:

[0028] 1) Carboxyl-terminated 5,15-bis(3-hydroxyphenyl)-10,20-diphenylporphyrin / polyethylene lactide / polyethylene glycol block copolymer with a molar ratio of 1:1 Mixed with RGD peptide, added with the carboxyl-terminated 5,15-bis(3-hydroxyphenyl)-10,20-diphenylporphyrin / polyethylene lactide / polyethylene glycol block copolymer The carboxyl-terminal equivalent carbodiimide cross-linking agent in the molecule was reacted at 20°C for 72 hours to connect the RGD peptide to the carboxyl-terminated 5,15-bis(3-hydroxyphenyl )-10,20-diphenylporphyrin / polyethylene lactide / polyethylene glycol block copolymer;

[0029] 2) Dis...

Embodiment 3

[0034] In Example 3, the selected carboxyl-terminated porphyrin-amphiphilic block copolymer is carboxyl-terminated 5,10,15-tris(3-hydroxyphenyl)-20-phenylporphyrin / Polyethylene lactide / polyethylene glycol block copolymer, the selected hydrophobic drug is desalted doxorubicin, and the steps for preparing RGD-targeted doxorubicin porphyrin polymer nanomicelle are as follows:

[0035] 1) Carboxyl-terminated 5,10,15-tris(3-hydroxyphenyl)-20-phenylporphyrin / polyethylene lactide / polyethylene glycol block copolymer with a molar ratio of 1:50 RGD peptide is mixed and added to the carboxyl-terminated 5,10,15-tris(3-hydroxyphenyl)-20-phenylporphyrin / polyethylene lactide / polyethylene glycol block copolymer molecule The carboxyl-terminal equivalent carbodiimide cross-linking agent was reacted at 30°C for 18 hours to connect the RGD peptide to the carboxyl-terminated 5,10,15-tri(3-hydroxyphenyl )-20-phenylporphyrin / polyethylene lactide / polyethylene glycol block copolymer;

[0036] 2) Di...

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Abstract

The invention discloses a preparation method for RGD-targeted porphyrin polymer nanomicelle. The preparation method comprises the following steps: firstly, connecting an RGD to a porphyrin-amphiphilic block copolymer by an amido bond; secondly, dissolving the product prepared in the first step and a hydrophobic drug into acetone; thirdly, adding the solution prepared in the second step into an aqueous solution, stirring to volatilize and removing the acetone; fourthly, centrifuging, collecting solidified nano particles, freezing and drying to obtain the RGD-targeted porphyrin polymer nanomicelle. The RGD-targeted porphyrin polymer nanomicelle disclosed by the invention integrates an active tumor targeting function, phototherapy-chemotherapy function and a tumor resisting function and has photosensitive activity and antitumor activity for further loading a chemical medicament; the tumor treatment effect can be enhanced under the synthetic actions of active targeting and tumor resistance.

Description

technical field [0001] The invention relates to a preparation method of nano micelles, in particular to a preparation method of polymer nano micelles. Background technique [0002] With the aging of society and the change of people's lifestyle, malignant tumor has become the "first killer" of human beings. Clinically available tumor treatment methods include surgery, chemotherapy, radiotherapy, photodynamic therapy, and hyperthermia. The multi-inducing factors of cancer lead to poor efficacy of any single treatment, and the mortality rate is still year by year. rise. The use of multi-method comprehensive treatment of tumors to achieve synergy and complementarity between different treatment methods will greatly improve the anti-tumor efficacy and increase the survival rate of patients, which is a new trend in the treatment of malignant tumors. The emergence of nanomedicine provides an ideal functional platform for multi-means comprehensive treatment of tumors. [0003] Tum...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K41/00A61K9/19A61P35/00
Inventor 马桂蕾宋存先
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI