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Province","doi-asserted-by":"publisher","award":["212300410057"],"award-info":[{"award-number":["212300410057"]}],"id":[{"id":"10.13039\/501100006407","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100006407","name":"Natural Science Foundation of Henan Province","doi-asserted-by":"publisher","award":["29"],"award-info":[{"award-number":["29"]}],"id":[{"id":"10.13039\/501100006407","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100006407","name":"Natural Science Foundation of Henan Province","doi-asserted-by":"publisher","award":["222300420482"],"award-info":[{"award-number":["222300420482"]}],"id":[{"id":"10.13039\/501100006407","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Triptolide (TP) is a potential drug candidate for the treatment of cancer, but its use was hampered by its systemic toxicity and poor water solubility. Hence, a TP-CSO prodrug was synthesized by conjugating TP to chitosan oligosaccharide (CSO), and characterized by 1H NMR, FTIR, DSC and XRD analyses. The TP-CSO containing about 4 wt% of TP exhibited excellent water solubility (15 mg\/mL) compared to TP (0.017 mg\/mL). Compared with TP, the pharmacokinetics of the conjugate after oral administration showed a three-fold increase in the half-life in the blood circulation and a 3.2-fold increase in AUC (0\u2013\u221e). The orally administered TP-CSO could more effectively inhibit tumor progression but with much lower systemic toxicity compared with TP, indicating significant potential for further clinical trials. In conclusion, CSO-based conjugate systems may be useful as a platform for the oral delivery of other sparingly soluble drugs.<\/jats:p>","DOI":"10.3390\/molecules27123686","type":"journal-article","created":{"date-parts":[[2022,6,12]],"date-time":"2022-06-12T22:37:20Z","timestamp":1655073440000},"page":"3686","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["TP-CSO: A Triptolide Prodrug for Pancreatic Cancer Treatment"],"prefix":"10.3390","volume":"27","author":[{"given":"Xinlong","family":"Wang","sequence":"first","affiliation":[{"name":"Academy of Chinese Medicine Sciences, Henan University of Chinese Medicine, Zhengzhou 450046, China"},{"name":"Pharmacy College, Henan University of Chinese Medicine, Zhengzhou 450046, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Huahui","family":"Zeng","sequence":"additional","affiliation":[{"name":"Academy of Chinese Medicine Sciences, Henan University of Chinese Medicine, Zhengzhou 450046, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xin","family":"Zhu","sequence":"additional","affiliation":[{"name":"Pharmacy College, Henan University of Chinese Medicine, Zhengzhou 450046, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Duanjie","family":"Xu","sequence":"additional","affiliation":[{"name":"Pharmacy College, Henan University of Chinese Medicine, Zhengzhou 450046, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Qikang","family":"Tian","sequence":"additional","affiliation":[{"name":"Pharmacy College, Henan University of Chinese Medicine, Zhengzhou 450046, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Can","family":"Wang","sequence":"additional","affiliation":[{"name":"Pharmacy College, Henan University of Chinese Medicine, Zhengzhou 450046, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lingzhou","family":"Zhao","sequence":"additional","affiliation":[{"name":"Department of Nuclear Medicine, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200080, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Junwei","family":"Zhao","sequence":"additional","affiliation":[{"name":"Department of Clinical Laboratory, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mingsan","family":"Miao","sequence":"additional","affiliation":[{"name":"Academy of Chinese Medicine Sciences, Henan University of Chinese Medicine, Zhengzhou 450046, China"},{"name":"Pharmacy College, Henan University of Chinese Medicine, Zhengzhou 450046, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3623-1161","authenticated-orcid":false,"given":"Xiangxiang","family":"Wu","sequence":"additional","affiliation":[{"name":"Academy of Chinese Medicine Sciences, Henan University of Chinese Medicine, Zhengzhou 450046, China"},{"name":"Pharmacy College, Henan University of Chinese Medicine, Zhengzhou 450046, China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2022,6,8]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"4846","DOI":"10.3748\/wjg.v24.i43.4846","article-title":"Pancreatic cancer: A review of clinical diagnosis, epidemiology, treatment and outcomes","volume":"24","author":"McGuigan","year":"2018","journal-title":"World J. 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