Preparation and characteristics of 10-hydroxycamptothecin loaded folate-receptor targeted phase-change contrast agent / 中国介入影像与治疗学

ABSTRACT

Objective To prepare a 10-hydroxycamptothecin (10-HCPT) loaded folate-receptor targeted phase-change contrast agent (FR-HCPT-PNPCA),and to study the general characteristics including drug loading,phase changing and targeting capability in vitro.Methods Using a method of two-step emulsification,the phase-change nanoparticles loading anticancer drug (10-HCPT) with lipids shell and liquid pefluorocarbon core were prepared.The entrapment efficiency and the drug-loading amounts were studied by high performance liquid chromatography,and the phase transition of the nanoparticles after heating was observed.The targeting ability was evaluated on liver cancer cell line 7721 in vitro.Results The FR-HCPT-PNPCA,with a drug encapsulation rate of about 70.42 ％ and drug loading amounts of about 20.05 ％,was prepared successfully.When being heated to 70℃,obvious phase changing and microbubbles generating could be observed under microscope.In addition,a large amount of FR-HCPT-PNPCA particles could adhere specifically around the 7721 cells.Conclusion The prepared FR-HCPT-PNPCA,which has a stable characteristic and high performance of drug loading and tumor targeting,is expected to become a promising multifunctional molecular ultrasound probe for diagnosis and treatment of tumor.