Cationic polymer-loaded paclitaxel/indocyanine green co-delivery micelle and preparation method thereof

A cationic polymer, indocyanine green technology, used in drug combinations, pharmaceutical formulations, emulsion delivery and other directions

Inactive Publication Date: 2015-12-30
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Previous drug carriers have not fully combined these new technologies, and tumor therapy and imaging are still two independent concepts

Method used

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  • Cationic polymer-loaded paclitaxel/indocyanine green co-delivery micelle and preparation method thereof
  • Cationic polymer-loaded paclitaxel/indocyanine green co-delivery micelle and preparation method thereof

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Embodiment Construction

[0021] The specific steps for the synthesis and preparation of paclitaxel / ICG / polyethylene glycol-polycaprolactone-polyethyleneimine (PTX / ICG / PEG-PCL-PEI) cationic nanomicelle complex are as follows:

[0022] Taking the synthesis of each block with molecular weights of MWMPEG5000, MWPCL2000, and MWPEI2000 as an example, polymers with different block ratios and molecular weights were synthesized separately. Synthetic route such as figure 1 Shown:

[0023] 1. Add anhydrous MPEG (2kDa~5kDa) into a three-necked flask, weigh caprolactone (1.2:1 molar ratio to MPEG), drop into stannous octoate (0.5%w / w), heat the oil bath to 130 ℃, magnetically stirred and reacted under nitrogen protection conditions for 6 hours, cooled in vacuo, dissolved the reaction mixture with dichloromethane, and repeatedly precipitated and washed with pre-cooled petroleum ether to obtain MPEG-PCL;

[0024] 2. Dry MPEG-PCL and dissolve it with anhydrous dichloromethane. After adding 3 drops of triethylamine ...

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Abstract

The invention provides a cationic polymer-loaded paclitaxel/indocyanine green (ICG) co-delivery micelle and a preparation method thereof. To simultaneously load the chemotherapeutic paclitaxel and the photosensitizer ICG, an amphiphilic degradable cationic nano-micelle MPEG-PCL-PEI is used as a loading medium for the chemotherapeutic paclitaxel; a cationic polymer block is introduced into a polymer MPEG-PCL which forms the nano-micelle, so surface charges of the micelle can be changed; negatively-charged ICG molecules are adsorbed through interaction between positive and negative charges, and sustained release of paclitaxel and ICG is realized; so a novel method is provided for integrated diagnosis and treatment of tumors. According to the invention, the triblock cationic polymer synthesized from an amphiphilic polymer-grafted cationic fragment can simultaneously load the chemotherapeutic paclitaxel and the photosensitizer ICG approved by FDA, so compounding of the chemotherapeutic and fluorescence molecules is realized, and fluorescent imaging of a tumor site as well as target drug delivery for a tumor is complished.

Description

technical field [0001] The invention relates to the field of tumor diagnosis and treatment integration, in particular to cationic polymer-loaded paclitaxel / indocyanine green co-transport micelles and a preparation method thereof. Background technique [0002] The continuous development of functional polymers has promoted the development of new drug delivery systems in pharmacy, making anti-tumor drugs and methods constantly improved. Among most anti-tumor clinical first-line drugs, chemical small-molecule drugs have been widely used and have relatively high toxic and side effects. core issues of treatment. [0003] Paclitaxel, a conventional chemotherapy drug, inhibits cell mitosis by promoting tubulin polymerization and inhibiting its depolymerization. In clinical use, it is suitable for ovarian cancer, breast cancer, and also has curative effects on lymph cancer, intestinal cancer and lung cancer. At the same time, as a fat-soluble compound, paclitaxel has been prepared ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K9/107A61K47/34A61K31/337A61P35/00A61K49/00
Inventor 师帅李星熠赵文光陈浩
Owner WENZHOU MEDICAL UNIV
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