A series of drugs for tumor photodynamic therapy and its application

Abstract

The invention belongs to the field of nano drug preparations, and relates to a series of drugs for tumor photodynamic therapy and applications thereof. The series of drugs include drug A and drug B, the drug A is TGF-beta inhibitor LY2157299, and the drug B is a nano-medicine of a conjugate of hydroxyethyl starch grafted with chlorin e6. In the present invention, LY2157299 is combined with hydroxyethyl starch-coupled chlorin e6 nano-medicine, and applied to tumor photodynamic therapy. LY2157299 can improve tumor extracellular matrix, reduce solid stress, reduce the compression of blood vessels, and promote nano-medicine and due to the specific multi-branched structure of the carrier hydroxyethyl starch of the nanomedicine used in the present invention, it greatly reduces the aggregation of the photosensitizer when it is coupled with chlorin e6 and can be used at an extremely low loading The higher active oxygen production rate can be obtained by the dose, and the toxic and side effects of the drug are greatly reduced on the basis of ensuring the photodynamic efficacy.

Description

technical field [0001] The invention belongs to the field of nano-pharmaceutical preparations, and relates to a series of drugs for photodynamic therapy of tumors and applications thereof, more specifically, relates to a combination of TGF-beta inhibitors and nano-medicines and their application in the preparation of drugs for photodynamic therapy of tumors. Background technique [0002] Currently, photodynamic therapy (PDT) is widely used in antitumor research. Photodynamic therapy is a minimally invasive therapy clinically approved by the Food and Drug Administration (FDA), which can selectively kill malignant tumors. Photodynamic therapy consists of three parts: photosensitizer, oxygen and light. The three parts work together to generate active oxygen, thereby killing tumors and achieving anti-tumor effects. However, most photosensitizers, such as chlorin e6, are poorly soluble in water and lack targeting, so they cannot be targeted to tumors. Aggregation of chlorin e6 ...

AI Technical Summary

Problems solved by technology

However, most photosensitizers, such as chlorin e6, are poorly soluble in water and lack targeting to tumors

Aggregation of chlorin e6 in aqueous solution results in reduced reactive oxygen species production, limiting the antitumor application of photodynamic therapy

Although polyethylene glycol can improve the water solubility and targeting of chlorin e6 and increase the yield of reactive oxygen species to a certain extent, the yield of reactive oxygen species in polyethylene glycol-grafted chlorin e6 nanomedicine remains to be seen. In addition, in order to increase the active oxygen production rate of polyethylene glycol chlorin e6 conjugates, it is necessary to increase the amount of chlorin e6 used, and the high amount of use will lead to the toxicity of photosensitizer chlorin e6 to normal tissues. Enhanced side effects

[0004] On the other hand, there is also a dense extracellular matrix at the tumor site, which hinders drug delivery to the tumor

Compared with immunotherapy or chemotherapeutic drugs, photodynamic therapy has the biggest advantage of less side effects on tumor patients. However, it also has defects such as poor therapeutic effect and easy recurrence of the disease, mainly due to insufficient drug delivery, and The active oxygen yield of the drug is too low during photodynamic therapy, especially due to the low active oxygen yield of the nanomedicine targeting the tumor site.

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