Strategies for Solubility and Bioavailability Enhancement and Toxicity Reduction of Norcantharidin
Cantharidin (CTD) is the main active ingredient isolated from Mylabris, and norcantharidin (NCTD) is a demethylated derivative of CTD, which has similar antitumor activity to CTD and lower toxicity than CTD. However, the clinical use of NCTD is limited due to its poor solubility, low bioavailability...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-11-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/22/7740 |
| _version_ | 1797464405571534848 |
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| author | Qian Liu Henglai Sun Xinyu Li Huagang Sheng Liqiao Zhu |
| author_facet | Qian Liu Henglai Sun Xinyu Li Huagang Sheng Liqiao Zhu |
| author_sort | Qian Liu |
| collection | DOAJ |
| description | Cantharidin (CTD) is the main active ingredient isolated from Mylabris, and norcantharidin (NCTD) is a demethylated derivative of CTD, which has similar antitumor activity to CTD and lower toxicity than CTD. However, the clinical use of NCTD is limited due to its poor solubility, low bioavailability, and toxic effects on normal cells. To overcome these shortcomings, researchers have explored a number of strategies, such as chemical structural modifications, microsphere dispersion systems, and nanodrug delivery systems. This review summarizes the structure–activity relationship of NCTD and novel strategies to improve the solubility and bioavailability of NCTD as well as reduce the toxicity. This review can provide evidence for further research of NCTD. |
| first_indexed | 2024-03-09T18:07:39Z |
| format | Article |
| id | doaj.art-1c7b39c060ba408ea2f8636ff00bf449 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T18:07:39Z |
| publishDate | 2022-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-1c7b39c060ba408ea2f8636ff00bf4492023-11-24T09:20:31ZengMDPI AGMolecules1420-30492022-11-012722774010.3390/molecules27227740Strategies for Solubility and Bioavailability Enhancement and Toxicity Reduction of NorcantharidinQian Liu0Henglai Sun1Xinyu Li2Huagang Sheng3Liqiao Zhu4College of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250355, ChinaCollege of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250355, ChinaCollege of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250355, ChinaCollege of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250355, ChinaCollege of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250355, ChinaCantharidin (CTD) is the main active ingredient isolated from Mylabris, and norcantharidin (NCTD) is a demethylated derivative of CTD, which has similar antitumor activity to CTD and lower toxicity than CTD. However, the clinical use of NCTD is limited due to its poor solubility, low bioavailability, and toxic effects on normal cells. To overcome these shortcomings, researchers have explored a number of strategies, such as chemical structural modifications, microsphere dispersion systems, and nanodrug delivery systems. This review summarizes the structure–activity relationship of NCTD and novel strategies to improve the solubility and bioavailability of NCTD as well as reduce the toxicity. This review can provide evidence for further research of NCTD.https://www.mdpi.com/1420-3049/27/22/7740norcantharidinsolubilitybioavailabilityantitumorstructural modificationnanopreparation |
| spellingShingle | Qian Liu Henglai Sun Xinyu Li Huagang Sheng Liqiao Zhu Strategies for Solubility and Bioavailability Enhancement and Toxicity Reduction of Norcantharidin Molecules norcantharidin solubility bioavailability antitumor structural modification nanopreparation |
| title | Strategies for Solubility and Bioavailability Enhancement and Toxicity Reduction of Norcantharidin |
| title_full | Strategies for Solubility and Bioavailability Enhancement and Toxicity Reduction of Norcantharidin |
| title_fullStr | Strategies for Solubility and Bioavailability Enhancement and Toxicity Reduction of Norcantharidin |
| title_full_unstemmed | Strategies for Solubility and Bioavailability Enhancement and Toxicity Reduction of Norcantharidin |
| title_short | Strategies for Solubility and Bioavailability Enhancement and Toxicity Reduction of Norcantharidin |
| title_sort | strategies for solubility and bioavailability enhancement and toxicity reduction of norcantharidin |
| topic | norcantharidin solubility bioavailability antitumor structural modification nanopreparation |
| url | https://www.mdpi.com/1420-3049/27/22/7740 |
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