title: [Preparation and in vitro properties of folate receptor targeting docetaxel-loaded amphiphilic copolymer-modified liposomes].
abstract: A novel amphiphilic copolymer, folate-poly (PEG-cyanoacrylate-co-cholesteryl cyanoacrylate) (FA-PEG-PCHL) was synthesized as liposomal modifying material with folate receptor targeting and long circulating property. FA-PEG-PCHL-modified docetaxel-loaded liposomes (FA-PDCT-L) were prepared by organic solvent injection method, and the system was optimized using central composite design-response surface methodology. The structure of the FA-PEG-PCHL copolymer was confirmed by FT-IR and 1H NMR. Ultrafiltration technique, transmission electron microscope, dynamic light scattering and electrophoretic light scattering, and fluorescence polarization method were used to study the physicochemical parameters of FA-PDCT-L. FA-PDCT-L showed spherical or ellipsoid shape. The mean particle sizes were in the range of 111.6-126.9 nm, zeta potentials were from -6.54 mV to -14.13 mV and the drug encapsulation efficiency achieved 97.8%. The observed values agreed well with model predicted values. The membrane fluidity increased with the increment of the molecular weight of PEG and the decrement of the amount of FA-PEG-PCHL. The in vitro release test showed that the drug could be sustained-released from liposomes without a burst release and with stability for 6 months. After 24 h only 31.1%, 27.2% and 19.5% of encapsulated docetaxel were released for FA-PDCT10000-L, FA-PDCT4000-L and FA-PDCT2000-L, respectively. This work is useful for further research on the application of the synthesized copolymer-modified long circulating liposomes for cancer therapy.
authors.affiliation: National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Traditional Chinese Medicine, Nanchang 330006, China.
authors.forename: Xiang
authors.initials: X
authors.lastname: Li
authors.forename: Jing
authors.initials: J
authors.lastname: Zhang
authors.forename: Dong-Kai
authors.initials: DK
authors.lastname: Wang
authors.forename: Wei-San
authors.initials: WS
authors.lastname: Pan
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage*; D002788:Cholesterol Esters / Q000737:chemistry; D003487:Cyanoacrylates / Q000737:chemistry; D003692:Delayed-Action Preparations; D000077143:Docetaxel; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry; D016503:Drug Delivery Systems; D058973:Folate Receptors, GPI-Anchored / Q000737:chemistry; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry; D008970:Molecular Weight; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D011108:Polymers / Q000138:chemical synthesis / Q000737:chemistry; D043823:Taxoids / Q000008:administration & dosage*
chemical_list: D000970:Antineoplastic Agents; D002788:Cholesterol Esters; D003487:Cyanoacrylates; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D058973:Folate Receptors, GPI-Anchored; D008081:Liposomes; D011108:Polymers; D043823:Taxoids; D000077143:Docetaxel; D011092:Polyethylene Glycols