Gemcitabine-loaded Folic Acid Tagged Liposomes: Improved Pharmacokinetic and Biodistribution Profile.
作者： Sambamoorthy Unnam , Venkataraju Makam Panduragaiah , Manjappa Arehalli Sidramappa , Bhanoji Rao Muddana Eswara
DOI: 10.2174/1567201815666181024112252
关键词:
摘要: BACKGROUND Gemcitabine (GEM) is found effective in the treatment of many solid tumors. However, its use restricted due to small circulation half-life, fast metabolism and low capacity for selective tumor uptake. Folate receptors (FRs) have been recognized as cellular surface markers, which can be used cancer targeting. PEGylated liposomes decorated with folic acid investigated several anticancer agents not only extend plasma half-life but also targeting via overexpressed on cell surface. OBJECTIVE Therefore, objective present study was prepare GEM-loaded tagged improve pharmacokinetics distribution GEM. METHODS The blank folate-targeted composed HSPC/DSPE-mPEG2000/DSPE-mPEG-Folic were prepared first by thin film hydration technique. GEM then loaded into remote loading optimized liposomal formulations evaluated vitro release using dialysis technique, HeLa uptake FACS cytotoxicity MTT dye reduction assay. comparative vivo pharmacokinetic biodistribution characteristics radiolabeled (99mTc-labeled) plain solution, all (conventional:CLs; stealth: SLs; folate targeted: FTLs) mice model. RESULTS FTLs showed sustained profile, efficient cells greater cytotoxicity. Further, displayed significantly improved pharmacokinetics, profile CONCLUSION In conclusion, developed receptor-targeted formulation could a promising potential alternative further development.
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