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Synthesis and characterization of ramose tetralactosyl-lysyl-chitosan-5-fluorouracil and its in vitro release

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Abstract

In order to improve drug loading and achieve a good release effect, this paper adopts the ramose method, choosing chitosan as the carrier and 5-fluorouracil (5-Fu) as a model drug. Ramose chitosan-lysyl-5-Fu(3) and ramose tetralactosyl-lysyl-chitosan-5-Fu(6) were synthesized successfully, then the in vitro release of (6) was researched. The results show that the drug loading of (3) and (6) are 9.17 and 1.63% (w/w), respectively. The in vitro release behavior of (6) in pH 7.4 phosphate buffer solution and pH 1.2 HCl–KCl solution were studied. The zero order release time that (6) maintains in alkaline and acidic media are 64 and 24 h, and the total release by 184 h are 71.97 and 82.34%, respectively. The performance is smooth throughout the whole stage of release, and the concentration of cumulative release is lower in the alkaline environment than in the acidic environment over the same time.

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Acknowledgments

This work was supported by the National Natural Science Foundation of China (No. 20775010), the Natural Science Foundation of Hunan Province of China (06JJ2038) and the Graduate Innovation Fund of Hunan Province of China.

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Correspondence to He-ping Li.

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Li, Hp., Qin, L., Wang, Zd. et al. Synthesis and characterization of ramose tetralactosyl-lysyl-chitosan-5-fluorouracil and its in vitro release. Res Chem Intermed 38, 1421–1429 (2012). https://doi.org/10.1007/s11164-011-0473-x

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  • DOI: https://doi.org/10.1007/s11164-011-0473-x

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