一种刺激响应型胆碱磷酸脂质分子及其制法和应用

By designing stimulus-responsive choline phospholipid molecules, the problems of existing liposome drug delivery complexes lacking structural modification sites and having poor targeting were solved, enabling controlled drug release and tumor targeting, improving drug utilization and reducing toxic side effects.

CN116874523BActive Publication Date: 2026-07-17SOUTHEAST UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SOUTHEAST UNIV
Filing Date
2023-05-11
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing liposome-loaded drug complexes lack structural modification sites, resulting in poor targeting and a lack of responsiveness to environmental stimuli, leading to low drug utilization and significant toxic side effects.

Method used

We designed a stimulus-responsive choline phospholipid molecule by introducing thioether or thioacetate groups into the hydrophobic chain portion, enabling it to release drugs in response to specific environments and achieve targeting by attracting the cell membrane through an inverted PC configuration.

Benefits of technology

It achieves controlled drug release and tumor targeting, improves drug utilization, reduces toxic side effects, and has broad application prospects in tumor treatment.

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Abstract

本发明公开了一种刺激响应型胆碱磷酸脂质分子，还公开了上述刺激响应型胆碱磷酸脂质分子的制备方法及其用于制备载药脂质体复合物方面的应用。本发明脂质体，L左侧为疏水链部分、右侧为胆碱磷酸结构，二者以特定的L基团连接，形成特定结构的脂质分子，在A1和A2疏水双链处引入硫醚、缩硫酮或二硫键刺激响应基团，在疏水双链中含有刺激响应基团通过引起脂质体疏水性(疏水性变成亲水性)的改变，从而快速地释放出所包载物；胆碱磷酸的R基团可被选择性修饰，从而能够得到不同种类、不同功能的脂质体；本发明脂质体具有刺激响应性和肿瘤靶向性，制备的载药脂质体复合物表现出对肿瘤生长的显著抑制作用，从而在肿瘤治疗方面具有广阔的应用前景。
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