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J Drug Target ; 26(4): 345-356, 2018 04.
Artigo em Inglês | MEDLINE | ID: mdl-28920483

RESUMO

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.


Assuntos
Camptotecina/análogos & derivados , Carcinoma Hepatocelular/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Neoplasias Hepáticas/tratamento farmacológico , Animais , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/farmacocinética , Antineoplásicos Fitogênicos/farmacologia , Camptotecina/administração & dosagem , Camptotecina/farmacocinética , Camptotecina/farmacologia , Carcinoma Hepatocelular/patologia , Linhagem Celular Tumoral , Portadores de Fármacos/química , Humanos , Lipossomos , Neoplasias Hepáticas/patologia , Magnetismo , Masculino , Camundongos , Microdiálise , Ratos , Ratos Sprague-Dawley , Temperatura
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