[關(guān)鍵詞]
[摘要]
7-乙基-10-羥基喜樹堿（SN38）是伊立替康的活性代謝物，在體外的抗腫瘤效果是伊立替康的100～1 000倍。然而，SN38水溶性差、在pH＞9.0時(shí)完全水解開環(huán)為不具有治療效果的羧酸鹽形式。SN38新型給藥系統(tǒng)均可提高藥物在各種不同癌癥模型中的理化性質(zhì)和體內(nèi)性能，從而提高其抗腫瘤活性和減少不良反應(yīng)。因此從物理封裝、化學(xué)偶聯(lián)和主動(dòng)腫瘤靶向3種策略對基于SN38的新型給藥系統(tǒng)進(jìn)行介紹，為后續(xù)開發(fā)出有效SN38新型給藥系統(tǒng)提供參考。
[Key word]
[Abstract]
7-Ethyl-10-hydroxycamptothecin (SN38), the active metabolite of irinotecan, has 100-1 000 times the antitumor effect of irinotecan in vitro. However, SN38 has poor water solubility, and when pH > 9.0, it was completely hydrolyzed and ring opened into the form of carboxylate without therapeutic effect. The novel SN38 drug delivery system could improve the physicochemical properties and in vivo performance of drugs in various cancer models, thereby enhancing anti-tumor activity and reducing adverse reactions. This article introduces the novel drug delivery system of SN38 from three strategies:physical encapsulation, chemical coupling, and active tumor targeting, to provide reference for the subsequent development of effective SN38 novel drug delivery systems.
[中圖分類號]
R944
[基金項(xiàng)目]
國家自然科學(xué)基金資助項(xiàng)目（81860630）；江西省重點(diǎn)研發(fā)計(jì)劃項(xiàng)目（20192ACB70012）；江西中醫(yī)藥大學(xué)1050計(jì)劃；南昌市重大科技攻關(guān)項(xiàng)目（2020-201-15）
