Application of 5-azacytosine in preparation of medicine for preventing and / or treating cervical intraepithelial neoplasia and microneedle patch of 5-azacytosine

By loading 5-azacytosine onto microneedle patches, the problems of invasiveness and low local delivery efficiency of existing treatment methods are solved, achieving non-invasive and effective treatment of cervical intraepithelial neoplasia.

CN122297503APending Publication Date: 2026-06-30SUN YAT SEN UNIVERSITY CANCER CENTER (CANCER HOSPITAL AFFILIATED TO SUN YAT SEN UNIVERSITY CANCER RESEARCH INSTITUTE OF SUN YAT SEN UNIVERSITY)
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Patent Information

Application Number
CN202610510007.0
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-04-17
Publication Date
2026-06-30

AI Technical Summary

Technical Problem

Existing treatments for cervical intraepithelial neoplasia, such as LEEP surgery, are highly invasive, leading to anatomical damage. Furthermore, traditional external drug administration has difficulty penetrating the cervical mucus layer, resulting in low local delivery efficiency. Systemic administration of 5-azacytosine nucleoside has significant toxic side effects.

Method used

The microneedle patch loaded with 5-azacytosine nucleoside is inserted into the cervical epithelium through a microneedle array layer made of biodegradable polymer material, achieving local delivery and continuous release, thus avoiding the toxic side effects of systemic administration.

Benefits of technology

It effectively inhibits and induces apoptosis of cervical intraepithelial neoplasia cells, reduces systemic toxicity, preserves fertility, and provides a non-invasive treatment option.

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Abstract

The invention belongs to the technical field of biological medicines, and discloses application of 5-azacytosine or a derivative or pharmaceutically acceptable salt thereof in preparation of a medicine for preventing and / or treating cervical intraepithelial neoplasia and a microneedle patch of the 5-azacytosine or the derivative or pharmaceutically acceptable salt thereof. In-vivo and in-vitro experiments prove that the 5-azacytosine or the pharmaceutically acceptable salt can remarkably inhibit growth and clone formation of cervical intraepithelial neoplasia cells and promote apoptosis of the cervical intraepithelial neoplasia cells, so that the 5-azacytosine or the pharmaceutically acceptable salt can be applied to preparation of the medicine for preventing and / or treating cervical intraepithelial neoplasia. The invention also provides a microneedle patch loaded with 5-azacytosine, and the 5-azacytosine is applied to a CIN lesion area, so that local precise delivery and continuous release are realized; the problems that the 5-azacytosine is easy to hydrolyze and open a ring, the toxic and side effects caused by systematic administration are high, and the traditional external administration is difficult to penetrate through a barrier to reach lesion penetration administration are solved, and the preparation has the advantages of minimally invasive property, high safety and good compliance.
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