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Hydroxycamptothecin liposomes based on thermal and magnetic dual-responsive system: preparation,in vitro and in vivo antitumor activity,microdialysis-based tumor pharmacokinetics
Authors:Hai-Mei Zhu  Jin-Hui Gu  Yi Xie
Institution:Department of pharmacy, College of Chinese Traditional Medicine, Guangzhou University of Chinese Medicine, Guangzhou, China
Abstract:Due to the absence of lactone form of hydroxycamptothecin, the commercially available hydroxycamptothecin injection exhibits inefficient therapeutic effects. In this study, we constructed a novel delivery system (thermosensitive magnetic liposomes) that protects lactone form of hydroxycamptothecin from blood or water. After hydroxycamptothecin was loaded into the thermosensitive magnetic liposome (HCPT/TML), its in vitro and in vivo antitumor activity and microdialysis-based tumour pharmacokinetics were determined. The results demonstrated that HCPT/TMLs possessed favourable physicochemical features and significant cytotoxicity against the Huh-7 cells in vitro. In the in vivo antitumor study and tumour pharmacokinetics, HCPT/TMLs displayed effective targeting delivery and antitumor effects, which corresponded to the determined hydroxycamptothecin concentration in tumour tissue. In conclusion, this thermal and magnetic dual-responsive system can efficiently deliver hydroxycamptothecin to tumour tissue and has great potential application in cancer treatment.
Keywords:Hydroxycamptothecin  liposomes  thermosensitive release  targeting delivery  pharmacokinetics  microdialysis  antitumor activity
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