Preparation of tumor-targeting chitosan micelle with transmembrane effect / 中国药科大学学报

ABSTRACT

Chitosan(CS)surface was modified with hydrophobic octyl groups to prepare N-octyl chitosan(nitro-gen-octyl chitosan;OC).Then hydrophilic group carboxyl-polyethylene glycol-amino (PEG);tumor-targeting lig-and D-glucosamine(DG);and membrane-penetrating peptide 9-D-arginine(9R)were linked to OC successively. Then the DG and 9R modified chitosan micelle (DG/9R-PEG-OC)with tumor-targeting and transmembrane effect was prepared.By hydrogen nuclear magnetic resonance spectrometer (1 H NMR)and sodium dodecyl sul-fate polyacryl amide gel electrophoresis(SDS-PAGE);the successful formation of DG/9R-PEG-OC was certified;with particle size of 151.8 nm and Zeta potential of 16.5 mV.The morphology of chitosan micelle observed by transmission electron microscope was homogeneous spherical structure.The drug loading content (DLC)(using fluorescein as a model drug)and encapsulation efficiency (EE)were about 28.2% and 75.0% measured by UV-visible spectrophotometer.Meanwhile;the drug showed a controlled releasing profile out of the micelle.Cellu-lar uptake experiments indicated DG/9 R-PEG-OC micelle had a significant tumor-tageting and transmembrane effects;especially on HepG2 cells;which exbihited high expression of the glucose transporter.Thus DG/9R-PEG-OC micelle could be a promising drug targeted delivery system of hydrophobic antitumor drugs.