Preparation, characterization and pharmacokinetics of N-palmitoyl chitosan anchored docetaxel liposomes.
The objective of this work was to investigate the preparation, characterization and pharmacokinetics of N-palmitoyl chitosan anchored docetaxel liposomes. To decrease toxic effects and improve antitumour efficacy of the drug, docetaxel has been incorporated in liposomes; the formulation, stability and pharmacokinetics of plain docetaxel liposomes (PDLs), PEGylated docetaxel liposomes (PEGDLs) and N-palmitoyl chitosan anchored docetaxel liposomes (NDLs) were compared. NDL was more stable than PDL and PEGDL in-vitro, especially in the presence of serum at 37 degrees C. The concentration of docetaxel in the plasma of rats after intravenous administration of docetaxel injection, PDL, PEGDL and NDL was studied by RP-HPLC. The pharmacokinetic behaviour of docetaxel injection, PDL, PEGDL and NDL were significantly different. These findings suggest that anchored liposomes could increase the stability of docetaxel in-vivo, as compared with plain liposomes, but the improvement was not more significant than PEGylated liposomes. N-Palmitoyl chitosan as a new polymeric membrane to anchor liposome was useful to stabilize liposomes containing anti-tumour drug.
Liang
Ge
G
School of Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu, 210009, PR China. Geliang.jiangyan@hotmail.com
Jia-Bi
Zhu
Z
Fei
Xiong
X
Bin
Ni
N
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D048271:Chitosan / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D000077143:Docetaxel; D016503:Drug Delivery Systems; D004355:Drug Stability; D007275:Injections, Intravenous; D008081:Liposomes; D008297:Male; D010316:Particle Size; D011092:Polyethylene Glycols; D051381:Rats; D017207:Rats, Sprague-Dawley; D017550:Spectroscopy, Fourier Transform Infrared; D043823:Taxoids / Q000008:administration & dosage / Q000493:pharmacokinetics*
D000970:Antineoplastic Agents; D008081:Liposomes; C510699:N-palmitoyl chitosan; D043823:Taxoids; D000077143:Docetaxel; D011092:Polyethylene Glycols; D048271:Chitosan