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19 Delivery of 1,2-dihydroquinolines via transferrin-targeted liposomes
  1. Yan Liu1,
  2. Robert J Lee1,2,
  3. Lesheng Teng1,
  4. Lirong Teng1
  1. 1School of Life Sciences, Jilin University, Changchun, China
  2. 2Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, OH, USA


Objectives Quinolines have been shown to have anticancer activities. This study investigates delivery of a novel quinolone using liposomes targeted to cancer cells.

Methods A 1, 2-dihydroquinoline was loaded into transferrin-targeted liposomes. Lipids (6.0 μmol), HSPC, cholesterol and PEG-DSPE in the ratio 63:36:1, and 0.5 μmol 1, 2-dihydroquinoline were dissolved in ethanol. An ethanol injection method was used to prepare transferrin-targeted liposomes. Mean particle size and ζ potential measurements, cytotoxicity assay, flow cytometry and confocal microscopy were performed.

Results The mean particle size of transferrin liposomes was 124 ± 2.7 nm. The ζ potential was −6 ± 1.2 mV. Transferrin-targeted liposomes showed high cytotoxicity for tumour cells. In competitive binding assays, the uptake from transferrin-targeted liposomes was inhibited 78% by 10 nM holo human transferrin. Flow cytometry and confocal microscopy analyses indicated that association of transferrin-targeted liposomes to tumour cells was much greater than that of non-targeted liposomes.

Conclusions We have identified a 1, 2-dihydroquinoline as a potential anticancer agent. Furthermore, this compound can be efficiently loaded into transferrin-targeted liposomes for targeted delivery to tumour cells. These data suggest that transferrin-targeted liposomes carrying 1, 2-dihydroquinoline are a potential anticancer agent for clinical application.

Acknowledgements This research was supported by Jilin Province Science and Technology Development Program (Grant No. 20140311072YY) and Jilin Province Science and Technology Development Program (Grant No. 20150520141JH).

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