{"data":{"id":"10.6084/m9.figshare.c.2116151","type":"dois","attributes":{"doi":"10.6084/m9.figshare.c.2116151","prefix":"10.6084","suffix":"m9.figshare.c.2116151","identifiers":[],"alternateIdentifiers":[],"creators":[{"name":"Guofei Li","affiliation":[],"nameIdentifiers":[]},{"name":"Cuifang Cai","affiliation":[],"nameIdentifiers":[]},{"name":"Yingjie Qi","affiliation":[],"nameIdentifiers":[]},{"name":"Tang, Xing","nameType":"Personal","givenName":"Xing","familyName":"Tang","affiliation":[],"nameIdentifiers":[]}],"titles":[{"title":"Hydroxyethyl starch–10-hydroxy camptothecin conjugate: synthesis, pharmacokinetics, cytotoxicity and pharmacodynamics research"}],"publisher":"Figshare","container":{},"publicationYear":2014,"subjects":[{"subject":"Biochemistry"},{"subject":"Pharmacology"},{"subject":"Biotechnology"},{"subject":"39999 Chemical Sciences not elsewhere classified","subjectScheme":"FOR"},{"subject":"FOS: Chemical sciences","schemeUri":"http://www.oecd.org/science/inno/38235147.pdf","subjectScheme":"Fields of Science and Technology (FOS)"},{"subject":"FOS: Chemical sciences","subjectScheme":"Fields of Science and Technology (FOS)"},{"subject":"Immunology"},{"subject":"FOS: Clinical medicine","schemeUri":"http://www.oecd.org/science/inno/38235147.pdf","subjectScheme":"Fields of Science and Technology (FOS)"},{"subject":"FOS: Clinical medicine","subjectScheme":"Fields of Science and Technology (FOS)"},{"subject":"Cancer"}],"contributors":[],"dates":[{"date":"2015-12-05","dateType":"Created"},{"date":"2016-05-20","dateType":"Updated"},{"date":"2014","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"}],"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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