Hydroxycamptothecin liposomes based on thermal and magnetic dual-responsive system: preparation, in vitro and in vivo antitumor activity, microdialysis-based tumor pharmacokinetics

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

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

The study was funded by Science and Technology Planning Project of Guangdong Province (No. 2014A020210022).