{"data":{"id":"10.6084/m9.figshare.c.2116151.v1","type":"dois","attributes":{"doi":"10.6084/m9.figshare.c.2116151.v1","prefix":"10.6084","suffix":"m9.figshare.c.2116151.v1","identifiers":[],"alternateIdentifiers":[],"creators":[{"name":"Tang, Xing","nameType":"Personal","givenName":"Xing","familyName":"Tang","affiliation":[],"nameIdentifiers":[]},{"name":"Guofei Li","affiliation":[],"nameIdentifiers":[]},{"name":"Cuifang Cai","affiliation":[],"nameIdentifiers":[]},{"name":"Yingjie Qi","affiliation":[],"nameIdentifiers":[]}],"titles":[{"title":"Hydroxyethyl starch–10-hydroxy camptothecin conjugate: synthesis, pharmacokinetics, cytotoxicity and pharmacodynamics research"}],"publisher":"Figshare","container":{},"publicationYear":2015,"subjects":[{"subject":"Cancer"},{"subject":"Immunology"},{"subject":"FOS: Clinical medicine","schemeUri":"http://www.oecd.org/science/inno/38235147.pdf","subjectScheme":"Fields of Science and Technology (FOS)"},{"subject":"Chemistry"},{"subject":"Biotechnology"},{"subject":"Pharmacology"},{"subject":"Cell Biology"},{"subject":"Biochemistry"}],"contributors":[],"dates":[{"date":"2015-12-05","dateType":"Created"},{"date":"2015-12-05","dateType":"Updated"},{"date":"2015","dateType":"Issued"}],"language":null,"types":{"ris":"GEN","bibtex":"misc","citeproc":"article","schemaOrg":"Collection","resourceType":"Collection","resourceTypeGeneral":"Collection"},"relatedIdentifiers":[{"relationType":"IsSupplementTo","relatedIdentifier":"10.3109/10717544.2014.911394","relatedIdentifierType":"DOI"},{"relationType":"IsPreviousVersionOf","relatedIdentifier":"10.6084/m9.figshare.c.2116151","relatedIdentifierType":"DOI"}],"relatedItems":[],"sizes":[],"formats":[],"version":null,"rightsList":[{"rights":"CC-BY","rightsUri":"http://creativecommons.org/licenses/by/3.0/us"}],"descriptions":[{"description":"10-hydroxy camptothecin (10-HCPT) is an antitumor agent effective in the treatment of several solid tumors but its use is hampered by poor water solubility, low lactone stability, short plasma half-life and dose-limiting toxicity. In this study, 10-HCPT-hydroxyethyl starch (HES) conjugate was prepared to overcome these limits of 10-HCPT. The solubility of 10-HCPT conjugate was 0.72 mg/ml, about 100 times to free 10-HCPT. The 10-HCPT conjugate showed good sustained release effect in phosphate-buffered saline (PBS), rat plasma and liver homogenate. Meanwhile, 10-HCPT–HES conjugate achieved much lower IC\u003csub\u003e50\u003c/sub\u003e and higher cytotoxicity effects than the free 10-HCPT on Hep-3B liver cancer cells. The pharmacokinetics results of 10-HCPT–HES conjugate demonstrated that the biological half-life of 10-HCPT was increased from 10 min to 4.38 h and the bioavailability was 40 times higher than the commercial 10-HCPT injection. The pharmacodynamics results indicated that 10-HCPT–HES conjugate had a better antitumor efficiency against nude mouse with Hep-3B tumor than the commercial 10-HCPT injection, and the inhibition ratio of tumor was 83.9 and 27.8%, respectively, at the same administration dosage. These findings suggest that 10-HCPT–HES conjugate is a promising drug delivery system providing improved long circulating effect, greater stability and better antitumor effect.","descriptionType":"Abstract"}],"geoLocations":[],"fundingReferences":[],"xml":"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","url":"https://figshare.com/collections/Hydroxyethyl_s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