Preparation and in vitro properties of folate receptor targeting docetaxel-loaded amphiphilic copolymer-modified liposomes.
- Author:
Xiang LI
1
;
Jing ZHANG
;
Dong-Kai WANG
;
Wei-San PAN
Author Information
1. National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Traditional Chinese Medicine, Nanchang 330006, China.
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
administration & dosage;
Cholesterol Esters;
chemistry;
Cyanoacrylates;
chemistry;
Delayed-Action Preparations;
Drug Carriers;
chemical synthesis;
chemistry;
Drug Delivery Systems;
Folate Receptors, GPI-Anchored;
chemistry;
Liposomes;
administration & dosage;
chemistry;
Molecular Weight;
Particle Size;
Polyethylene Glycols;
chemistry;
Polymers;
chemical synthesis;
chemistry;
Taxoids;
administration & dosage
- From:
Acta Pharmaceutica Sinica
2012;47(9):1219-1226
- CountryChina
- Language:Chinese
-
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.
