祝侠丽 李玲华 黄河清

[摘要]温敏脂质体是一种新型靶向药物载体。以温敏脂质体为载体包裹抗肿瘤药物，可利用肿瘤组织的滞留增强（EPR）效应将抗肿瘤药物载体靶向分布于肿瘤组织，然后结合局部外加热触发载体中的药物在肿瘤组织释放，可提高药物的靶向性，降低全身毒副作用，并可实现肿瘤的热化疗联合治疗。本研究通过查阅近年来国内外的相关文献，对温敏脂质体作为肿瘤靶向递药载体的研究进行综述。作为一种肿瘤靶向药物载体，温敏脂质体具有良好的应用前景。

[关键词]温敏脂质体；肿瘤靶向；递药载体

[中图分类号] R73-362 [文献标识码] A [文章编号] 1674-4721（2018）9（a）-0031-04

[Abstract] Thermosensitive liposome is a new targeted drug carrier. The thermosensitive liposome is used as a carrier to encapsulate an anti-tumor drug， which can be distributed to tumor tissues on targeting by utilizing an enhanced permeability and retention effect of the tumor tissue. After that， the drugs in the carrier will be released into tumor tissues once triggered by local external heating， which can improve the drug targeting， reduce systemic side effects， and achieve combined therapy of tumor thermochemotherapy. In this research， the related literature at home and abroad in recent years and the studies of thermosensitive liposomes as tumor-targeted drug delivery carriers were reviewed. As a tumor-targeted drug carrier， thermosensitive liposome has a good prospect.

[Key words] Thermosensitive liposome； Tumor targeting； Drug delivery carrier

脂质体（liposomes）作为一种抗肿瘤药物载体，具有制备简单、安全性高、靶向性强等优点，在临床上已逐渐开展应用。如何进一步提高脂质体的靶向性，并促进药物在靶组织的快速释药，是近年来该载体研究的热点。采用温敏脂质体（thermosensitive liposomes，TSL）包裹抗肿瘤药物并结合肿瘤组织的局部升温，实现药物的靶向传递以及在靶快速释药已经成为一种崭新的研究策略[1-2]。本研究就温敏脂质体作为肿瘤靶向递药载体的研究进展进行综述。

1温敏脂质体与肿瘤治疗

温敏脂质体介导的肿瘤靶向热化疗是近年肿瘤热化疗的一个新方向。温敏脂质体可在高于生理体温的条件下迅速、有效地释放药物，又称热敏脂质体。构建脂质体的磷脂都有特定的相变温度（Tm），在低于Tm时，脂质保持稳定，达到Tm时，脂质体膜的流动性、通透性增加，促使包封的药物快速释放。……