Preparation and characterization of paclitaxel delivery system based on semi-solid lipid nanoparticles coated with poly (ethylene glycol).
The current formulation of paclitaxel causes significant side effects, so there is a need to develop a safer delivery system. In this study, novel semi-solid lipid nanoparticles (PEG-PE-SSLN) were prepared, and evaluated as delivery vehicles for paclitaxel. The PEG-PE-SSLN are approximately 213 nm in size with a zeta-potential of -37 mV, compared to Span60-SSLN with a particle size of over 275 nm and zeta-potential of -29 mV. The encapsulation efficiency of PEG-PE-SSLN could be as high as 98%. Furthermore, differential scanning calorimetry (DSC) analysis indicated that paclitaxel in the nanoparticles existed in an amorphous form. A sustained release of 85% of the loaded paclitaxel from PEG-PE-SSLN within 12 days was observed while release from Span60-SSLN particles was complete within 6 days. PEG-PE-SSLN can effectively decrease phagocytosis of murine peritoneal macrophages. Lyopholization of SSLNs in the presence of trehalose tended to preserve their stability. Therefore, PEG-PE-SSLN represents an improved and promising paclitaxel delivery system.
Wu
Lifang
L
State Key Laboratory of Genetic Engineering, Department of Biochemistry, School of Life Sciences, Fudan University Shanghai, PR China. wlfang2008@sina.com
Tang
Cui
C
Yin
Chunhua
C
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D002851:Chromatography, High Pressure Liquid; D004339:Drug Compounding; D016503:Drug Delivery Systems; D007275:Injections, Intravenous; D008055:Lipids; D017737:Macrophages, Peritoneal / Q000378:metabolism; D051379:Mice; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D017239:Paclitaxel / Q000008:administration & dosage* / Q000493:pharmacokinetics; D010316:Particle Size; D010587:Phagocytosis; D010592:Pharmaceutic Aids; D011092:Polyethylene Glycols; D012995:Solubility; D014018:Tissue Distribution
D000972:Antineoplastic Agents, Phytogenic; D008055:Lipids; D010592:Pharmaceutic Aids; D011092:Polyethylene Glycols; D017239:Paclitaxel