LHRHa aided liposomes targeting to human ovarian tumor cells: preparation and cellular uptake.
In this study, a synthetic nonapeptide similar to luteinizing hormone-releasing hormone (LHRHa), the ligand of an extracellular membrane receptor specific to ovarian tumor cells, was selected as targeting moiety and electrically adsorbed to the negatively charged liposomes composed of phospholipid and monocholesterolsuccinate. Docetaxel, as the first line chemotherapy for ovarian tumor, was chosen to be encapsulated into the liposomes. And a high encapsulate efficiency (93%) and drug loading efficiency (20%) of liposomes were achieved via central composite design. In order to investigate the targeting efficiency of the drug delivery system, in vitro cell uptake was determined and the results showed an increasing uptake of LHRHa aided liposomes compared to normal ones.
Yuan
Wen-Min
WM
Key Laboratory of Drug Targeting and Novel Drug Delivery Systems, West China School of Pharmacy, Sichuan University Chengdu, China.
Song
Qin-Guo
QG
Zhang
Zhi-Rong
ZR
Fu
Yao
Y
Liu
Ji
J
He
Qin
Q
D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002788:Cholesterol Esters / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D000077143:Docetaxel; D004339:Drug Compounding; D016503:Drug Delivery Systems; D004563:Electrochemistry; D005260:Female; D019793:Fluorescein; D005453:Fluorescence; D006801:Humans; D008081:Liposomes; D007986:Luteinizing Hormone / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D010051:Ovarian Neoplasms / Q000188:drug therapy*; D012015:Reference Standards; D012044:Regression Analysis; D043823:Taxoids / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*
D000972:Antineoplastic Agents, Phytogenic; D002788:Cholesterol Esters; D008081:Liposomes; D043823:Taxoids; D000077143:Docetaxel; D007986:Luteinizing Hormone; C013440:cholesteryl succinate; D019793:Fluorescein