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Conjugate, targeted tumor active oxygen responsive medicine carrying nano-micelle as well as preparation methods and application thereof

A drug-loaded nano-conjugate technology, applied in the field of medicine, can solve the problems of lack of specific recognition ability of tumor tissue, difficulty in achieving therapeutic effect, and limited penetration ability, and achieve good biocompatibility, low cost, and improved targeted effect

Inactive Publication Date: 2018-09-28
STOMATOLOGICAL HOSPITAL TIANJIN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there are still many limitations in the use of PDT in the treatment of tumors: first, most photosensitizers have strong hydrophobicity, which makes it difficult to transport smoothly in the blood; second, photosensitizers lack the ability to specifically recognize tumor tissues , will produce phototoxicity to the normal tissue cells it enriches; third, the excitation light of most photosensitizers has a wavelength less than 700nm, and its penetration ability is limited, so it is difficult to achieve effective treatment for deep tumor tissues Effect

Method used

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  • Conjugate, targeted tumor active oxygen responsive medicine carrying nano-micelle as well as preparation methods and application thereof
  • Conjugate, targeted tumor active oxygen responsive medicine carrying nano-micelle as well as preparation methods and application thereof
  • Conjugate, targeted tumor active oxygen responsive medicine carrying nano-micelle as well as preparation methods and application thereof

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Embodiment 1

[0049] The present invention is described in detail by the following examples, they are only used to further illustrate the present invention, can not be interpreted as the limitation of protection scope of the present invention, those skilled in the art make some non-essential improvements and improvements according to the above-mentioned content of the present invention The adjustments all belong to the protection scope of the present invention.

[0050] Example 1:

[0051] 1. Synthesis and characterization of PTD

[0052] ① Dissolve carboxylated thioketal and mPEG in DMSO at a concentration of 5 mg / ml and 10 mg / ml, respectively, and then mix them at a molar ratio of 2:1, and rotate at 500 rpm for 36 hours under strict light-proof conditions. Subsequently, the reaction solution was transferred to a dialysis bag (molecular weight cut-off 500), and dialyzed in distilled water for 36 hours, and the water was changed once every 12 hours to remove DMSO and unreacted carboxylated...

Embodiment 2

[0087] 1. Preparation of mPEG-Thioketals-epirubicin (EPB) PTE

[0088] ① Dissolve carboxylated thioketal and mPEG in DMSO at concentrations of 5 mg / ml and 10 mg / ml, respectively, and then mix them at a molar ratio of 2:1, and rotate at 500 rpm for 36 hours under strict light-proof conditions. Subsequently, the reaction solution was transferred to a dialysis bag (molecular weight cut-off 500), and dialyzed in distilled water for 36 hours, and the water was changed every 12 hours to remove DMSO and unreacted carboxylated thioketal, and a white powder was obtained after freeze-drying The product mPEG-ketonethiol (PT).

[0089] ② Dissolve epirubicin (EPB) in DMSO at a concentration of 5 mg / ml, add three times the equivalent of triethylamine, and stir at room temperature for 12 hours at a speed of 500 rpm in the dark for desalination.

[0090]③Add the above desalted EPB into PT dissolved in DMSO at 5mg / ml, the molar ratio of EPB to PT is 1:1.5, and rotate at 500rpm for 36h under s...

Embodiment 3

[0096] 1. Preparation of mPEG-Thioketals-daunorubicin (DNR) PTD

[0097] ① Dissolve carboxylated thioketal and mPEG in DMSO at a concentration of 5 mg / ml and 10 mg / ml, respectively, and then mix them at a molar ratio of 2:1, and rotate at 500 rpm for 36 hours under strict light-proof conditions. Subsequently, the reaction solution was transferred to a dialysis bag (molecular weight cut-off 500), and dialyzed in distilled water for 36 hours, and the water was changed once every 12 hours to remove DMSO and unreacted carboxylated thioketal, and a white powder was obtained after freeze-drying The product mPEG-ketonethiol (PT).

[0098] ② Dissolve daunorubicin (DNR) in DMSO at a concentration of 5 mg / ml, add three times the equivalent of triethylamine, and stir at room temperature for 12 hours at a speed of 500 rpm in the dark for desalination.

[0099] ③Add the above desalted DNR into PT dissolved in DMSO at 5mg / ml, the molar ratio of DNR to PT is 1:1.5, and rotate at 500rpm for ...

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Abstract

The invention provides a targeted tumor active oxygen responsive medicine carrying nano-micelle, a preparation method and application of the medicine carrying nano-micelle, a medicine carrying nano-micelle intermediate RGD-PEG-thioketal-anthracene ring chemotherapy medicine conjugate and a preparation method of the conjugate. The nano-micelle, the conjugate as well as the preparation methods and application thereof have the beneficial effects that laser irradiates for activating porphyrin type photosensitive molecules; a large number of active oxygen radicals are triggered to be generated; further, thioketal in the medicine carrying nano-micelle system is induced to fracture; the controlled release of the anthracene ring chemotherapy medicine in the tumor position is realized; the medicinecurative effect is enhanced; the toxic and side effects of the medicine are reduced; PDT is combined with chemotherapy; the prominent synergistic interaction effect is achieved; the alone antitumor effect of a photodynamic therapy is improved; the toxic and side effects of the anthracene ring chemotherapy medicine on important visceral organs are also reduced.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a conjugate, a tumor-targeting reactive oxygen species-responsive drug-loaded nano-micelle, a preparation method and application thereof. Background technique [0002] Oral squamous cell carcinoma (OSCC) is the most common oral malignancy, and there are about 400,000 newly diagnosed patients with oral squamous cell carcinoma each year worldwide, with a high degree of malignancy, 5 The annual survival rate is less than 50%, which seriously threatens human life and health. Traditional tumor treatment methods have obvious disadvantages in the treatment of oral and maxillofacial tumors: surgical resection will inevitably affect the aesthetics of the maxillofacial region, and even cause damage to chewing, pronunciation, and swallowing functions; squamous cell carcinoma is poorly sensitive to chemotherapy drugs, Moreover, chemotherapy is also likely to cause damage to nor...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/704A61K41/00A61K47/60A61K47/62A61P35/00
Inventor 张连云王悦史澍睿王银松李长义张娟
Owner STOMATOLOGICAL HOSPITAL TIANJIN MEDICAL UNIV
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