Smart stimuli-responsive carrier-free nanoassembly of SN38 prodrug as efficient chemotherapeutic nanomedicine
The compound 7-ethyl-10-hydroxy-camptothecin (SN38) is a broad-spectrum antitumor agent whose applications are greatly limited by its poor solubility. Therefore, irinotecan, the hydrophilic derived prodrug of SN38, has been developed as the commercial formulation Campto ® for colorectal cancer. How...
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| Main Authors: | , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Compuscript Ltd
2023-01-01
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| Series: | Acta Materia Medica |
| Online Access: | https://www.scienceopen.com/hosted-document?doi=10.15212/AMM-2023-0003 |
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| author | Guanting Li Qianhui Jin Fengli Xia Shuwen Fu Xuanbo Zhang Hongying Xiao Chutong Tian Qingzhi Lv Jin Sun Zhonggui He Bingjun Sun |
| author_facet | Guanting Li Qianhui Jin Fengli Xia Shuwen Fu Xuanbo Zhang Hongying Xiao Chutong Tian Qingzhi Lv Jin Sun Zhonggui He Bingjun Sun |
| author_sort | Guanting Li |
| collection | DOAJ |
| description | The compound 7-ethyl-10-hydroxy-camptothecin (SN38) is a broad-spectrum antitumor agent whose applications are greatly limited by its poor solubility. Therefore, irinotecan, the hydrophilic derived prodrug of SN38, has been developed as the commercial formulation Campto ® for colorectal cancer. However, only 1% to 0.1% of irinotecan is converted to active SN38 in vivo, thus leading to unsatisfactory antitumor activity in clinical settings. Herein, we report a smart stimuli-responsive SN38 prodrug nanoassembly for efficient cancer therapy. First, SN38 was conjugated with an endogenous lipid, cholesterol (CST), via a redox dual-responsive disulfide bond (namely SN38-SS-CST). The prodrug self-assembled into uniform prodrug nanoassemblies with good colloidal stability and ultrahigh drug loading. SN38-SS-CST NPs released sufficient SN38 in the redox environments of tumor cells but remained intact in normal tissues. Finally, SN38-SS-CST NPs potently inhibited the growth of colon cancer without causing systemic toxicity, thus indicating their promise as a translational chemotherapeutic nanomedicine. |
| format | Article |
| id | doaj-art-ae6512a5df90477c8a75cb397dae81d1 |
| institution | OA Journals |
| issn | 2737-7946 |
| language | English |
| publishDate | 2023-01-01 |
| publisher | Compuscript Ltd |
| record_format | Article |
| series | Acta Materia Medica |
| spelling | doaj-art-ae6512a5df90477c8a75cb397dae81d12025-08-20T02:34:56ZengCompuscript LtdActa Materia Medica2737-79462023-01-0121546310.15212/AMM-2023-0003Smart stimuli-responsive carrier-free nanoassembly of SN38 prodrug as efficient chemotherapeutic nanomedicineGuanting LiQianhui JinFengli XiaShuwen FuXuanbo ZhangHongying XiaoChutong TianQingzhi LvJin SunZhonggui HeBingjun SunThe compound 7-ethyl-10-hydroxy-camptothecin (SN38) is a broad-spectrum antitumor agent whose applications are greatly limited by its poor solubility. Therefore, irinotecan, the hydrophilic derived prodrug of SN38, has been developed as the commercial formulation Campto ® for colorectal cancer. However, only 1% to 0.1% of irinotecan is converted to active SN38 in vivo, thus leading to unsatisfactory antitumor activity in clinical settings. Herein, we report a smart stimuli-responsive SN38 prodrug nanoassembly for efficient cancer therapy. First, SN38 was conjugated with an endogenous lipid, cholesterol (CST), via a redox dual-responsive disulfide bond (namely SN38-SS-CST). The prodrug self-assembled into uniform prodrug nanoassemblies with good colloidal stability and ultrahigh drug loading. SN38-SS-CST NPs released sufficient SN38 in the redox environments of tumor cells but remained intact in normal tissues. Finally, SN38-SS-CST NPs potently inhibited the growth of colon cancer without causing systemic toxicity, thus indicating their promise as a translational chemotherapeutic nanomedicine.https://www.scienceopen.com/hosted-document?doi=10.15212/AMM-2023-0003 |
| spellingShingle | Guanting Li Qianhui Jin Fengli Xia Shuwen Fu Xuanbo Zhang Hongying Xiao Chutong Tian Qingzhi Lv Jin Sun Zhonggui He Bingjun Sun Smart stimuli-responsive carrier-free nanoassembly of SN38 prodrug as efficient chemotherapeutic nanomedicine Acta Materia Medica |
| title | Smart stimuli-responsive carrier-free nanoassembly of SN38 prodrug as efficient chemotherapeutic nanomedicine |
| title_full | Smart stimuli-responsive carrier-free nanoassembly of SN38 prodrug as efficient chemotherapeutic nanomedicine |
| title_fullStr | Smart stimuli-responsive carrier-free nanoassembly of SN38 prodrug as efficient chemotherapeutic nanomedicine |
| title_full_unstemmed | Smart stimuli-responsive carrier-free nanoassembly of SN38 prodrug as efficient chemotherapeutic nanomedicine |
| title_short | Smart stimuli-responsive carrier-free nanoassembly of SN38 prodrug as efficient chemotherapeutic nanomedicine |
| title_sort | smart stimuli responsive carrier free nanoassembly of sn38 prodrug as efficient chemotherapeutic nanomedicine |
| url | https://www.scienceopen.com/hosted-document?doi=10.15212/AMM-2023-0003 |
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