Docetaxel polymer nano injection and preparation method thereof

Abstract

The invention provides a docetaxel polymer nano injection. The docetaxel polymer nano injection comprises the following components: modified docetaxel, a photosensitizer and a PH sensitive block, wherein the modified docetaxel is coated and modified by a shell cross-linked polymer; the modified docetaxel is connected with the photosensitizer through an acid sensitive bond; and the PH sensitive block coats the photosensitizer. The invention further provides a preparation method of the docetaxel polymer nano injection. According to the docetaxel polymer nano injection, the docetaxel has high stability while having high water solubility, is not liable to cause toxic and side effects of the whole body due to burst release, and can be slowly released; and meanwhile, chemotherapy and phototherapy are combined for treatment, so that the treatment effect on tumor cells can be effectively improved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a docetaxel polymer nano-injection and a preparation method thereof. Background technique [0002] Taxanes play an important role in the treatment of various solid tumors; docetaxel, a second-generation semi-synthetic taxane derivative, is about twice as effective as paclitaxel in participating in microtubule depolymerization, and can inhibit Cell division is mostly used to treat tumor diseases such as advanced breast cancer and non-small cell lung cancer. [0003] But the water solubility of docetaxel is poor, almost insoluble in water, prior art adopts Tween80 solubilization, ethanol solubilization to make pharmaceutical preparation; Because the existence of Tween80 makes this preparation in clinical use process can cause as allergic reaction, Severe adverse reactions such as neurotoxicity; and after docetaxel enters the body, the distribution is non-selective and reaches var...

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Problems solved by technology

[0003] But the water solubility of docetaxel is poor, almost insoluble in water, prior art adopts Tween80 solubilization, ethanol solubilization to make pharmaceutical preparation; Because the existence of Tween80 makes this preparation in clinical use process can cause as allergic reaction, Severe adverse reactions such as neurotoxicity; and after docetaxel enters the body, the distribution is non-selective and reaches various tissues and organs throughout the body, thereby causing systemic toxic and side effects, and easily causing toxicity to the nervous system and immune system, especially neutropenia Such as immune system toxicity, which greatly harms the physical and mental health of patients, which limits its clinical application; in addition, the stability of docetaxel is limited, and it must be used within 4 hours after clinical preparation, which limits the administration of docetaxel

[0004] At present, the existing technology solves the problem of poor water solubility of docetaxel by coating water-soluble polymer micelles on the surface of docetaxel, but its coating stability is still limited, and it will also be released suddenly when placed It is not highly resistant, it is inconvenient to apply, and it is easy to release suddenly after entering the body, which will bring systemic toxic and side effects; in addition, it is released too quickly after entering the body, and the therapeutic effect on tumor cells is not good.

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