Preparation and in vitro properties of folate receptor targeting docetaxel-loaded amphiphilic copolymer-modified liposomes / 药学学报
Acta Pharmaceutica Sinica
; (12): 1219-1226, 2012.
Article
in Zh
| WPRIM
| ID: wpr-274674
Responsible library:
WPRO
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.
Full text:
1
Index:
WPRIM
Main subject:
Particle Size
/
Polyethylene Glycols
/
Polymers
/
Drug Carriers
/
Chemistry
/
Cholesterol Esters
/
Drug Delivery Systems
/
Cyanoacrylates
/
Delayed-Action Preparations
/
Taxoids
Type of study:
Prognostic_studies
Language:
Zh
Journal:
Acta Pharmaceutica Sinica
Year:
2012
Type:
Article