Temperature-sensitive gel preparation containing glutaminase inhibitor as well as preparation method and application of temperature-sensitive gel preparation

By using a thermosensitive gel formulation under photothermal signal, it first releases glutaminase inhibitors to regulate the metabolism of the tumor microenvironment, and then releases immune checkpoint inhibitors to activate T cells, thus solving the problem of immunosuppression in the tumor microenvironment and achieving highly efficient anti-tumor immunotherapy.

CN121891291APending Publication Date: 2026-04-21CHINA PHARM UNIV
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Patent Information

Application Number
CN202610058702.8
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-01-16
Publication Date
2026-04-21

AI Technical Summary

Technical Problem

In current tumor immunotherapy, immune checkpoint inhibitors are not very effective due to immunosuppression caused by abnormally active glutamine metabolism in the tumor microenvironment.

Method used

Design a thermosensitive gel formulation comprising an outer gel layer and an inner gel layer, wherein the outer gel layer encapsulates the inner gel layer, the outer gel layer contains a glutaminase inhibitor and a photosensitizer, and the inner gel layer contains an immune checkpoint inhibitor. Drug release is controlled by photothermal signals, first releasing the glutaminase inhibitor to regulate metabolic state, and then releasing the immune checkpoint inhibitor to activate T cell immune response.

Benefits of technology

By regulating the metabolic state of the tumor microenvironment, immunosuppression can be alleviated, the effect of anti-tumor immunotherapy can be enhanced, and efficient tumor killing can be achieved.

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Abstract

The invention discloses a temperature-sensitive gel preparation containing a glutaminase inhibitor as well as a preparation method and application of the temperature-sensitive gel preparation, and belongs to the technical field of biological medicines. The temperature-sensitive gel preparation comprises outer-layer gel and inner-layer gel, the inner-layer gel is coated with the outer-layer gel, the outer-layer gel accounts for 40-75% of the total mass of the temperature-sensitive gel preparation, and the inner-layer gel accounts for 25-60% of the total mass of the temperature-sensitive gel preparation; the outer-layer gel is prepared from the following raw materials: an outer-layer gel matrix, a glutaminase inhibitor, a photosensitizer and a stabilizer; the raw materials of the inner-layer gel comprise an inner-layer gel matrix and an immune checkpoint inhibitor. According to the temperature-sensitive gel preparation, through photo-thermal control, the glutaminase inhibitor is firstly released to relieve the immunosuppression state, then the immune checkpoint inhibitor is released to kill tumors, and the glutaminase inhibitor and the immune checkpoint inhibitor act synergistically, so that efficient anti-tumor immunotherapy is achieved.
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