| The linoleic acid-grafted chitosan oligosaccharide(CSO-LA) polymeric micelles and chitosan oligosaccharide nanoparticles drug delivery systems for safety and better curative effect of anti-tumor drugs were prepared owing to the advantages of chitosan oligosaccharide including hypotoxicity,biodegradation and biocompatibility.The chemical conjugate of linoleic acid-grafted chitosan oligosaccharide(CSO-LA) was prepared in the presence of 1-ethyl-3-(3-dimethylaminoproyl) carbodiimide.DOX as a model drug,the size and zeta of DOX-loaded CSO-LA micelles(CSO-LA/DOX) were determined and the effects of the molecular weight of CSO and the graft ratio of LA on drug encapsulation efficiencies(EE),drug loading capacity(DL) and release behavior were also evaluated.Taking MCF-7,MCF-7/ADR,K562 and K562/ADR cells as modle cells,the cytotoxicity and cellular uptake of DOX·HCl,CSO-LA,as well as drug-loaded micelles(CSO-LA/DOX) in cells and the reversal effect of CSO-LA/DOX in MCF-7/ADR and K562/ADR cells were carried out.The results demonstrated that the CSO-LA micelles could not only improve the solubility and effect of hydrophobic anti-tumor drug,but also reverse the drug resistance of tumor cells.Because of the water-solubility and many amino groups of low molecular weight chitosan oligosaccharide,the paclitaxel loaded chitosan oligosaccharide nanoparticles were prepared by polyaddition polymerization in O/W miniemulsion system,and the particle size,drug entrapment efficiency and the in vitro drug release behavior could be controlled by the charged molar ratio of CSO to EGDE and the charged amount of CSO. |
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