Application of Paclitaxel-loaded EGFR Peptide-conjugated Magnetic Polymeric Liposomes for Liver Cancer Therapy.

Developing the methodologies that allow for safe and effective delivery of therapeutic drugs to target sites is a very important research area in cancer therapy. In this study, polyethylene glycol (PEG)-coated magnetic polymeric liposome (MPL) nanoparticles (NPs) assembled from octadecyl quaternized carboxymethyl chitosan (OQC), PEGylated OQC, cholesterol, and magnetic NPs, and functionalized with epithelial growth factor receptor (EGFR) peptide, were successfully prepared for in-vivo liver targeting. The two-step liver targeting strategy, based on both magnetic force and EGFR peptide conjugation, was evaluated in a subcutaneous hepatocellular carcinoma model of nude mouse. The results showed that EGFR-conjugated MPLs not only accumulated in the liver by magnetic force, but could also diffuse into tumor cells as a result of EGFR targeting. In addition, paclitaxel (PTX) was incorporated into small EGFR-conjugated MPLs (102.0±0.7 nm), resulting in spherical particles with high drug encapsulation efficiency (>90%). The use of the magnetic targeting for enhancing the transport of PTX-loaded EGFR-conjugated MPLs to the tumor site was further confirmed by detecting PTX levels. In conclusion, PTX-loaded EGFR-conjugated MPLs could potentially be used as an effective drug delivery system for targeted liver cancer therapy.

[Changes of colonic permeability and its correlation with TNF-α, NF-κB p65 in ulceration colitis mice].

OBJECTIVE: To study the changes of colonic permeability and its correlation with TNF-α, NF-κB p65 in indextran sulphate sodium (DSS) -induced ulcerative colitis(UC) of mice. METHODS: Forty-eight ICR mice were randomly divided into the control group and the model group. The acute UC model was induced by quantified intragastric administration of 2.5% DSS in mice. The disease activity index(DAI), histopathology scores, colonic permeability, expression of TNF-α, NF-κB p65 in colonic tissue were determined. The change of colonic permeability and its correlation with DAI, TNF-α, NF-κB p65 were analyzed. RESULTS: Compareded with the control group, DAI colonic permeability of colonic tissue,and the expression of TNF-α NF-κB p65 in the model group were increased significantly (P<0.01, P<0.01). The increased colonic permeability correlated with DAI (P<0.01), and the expression of TNF-α(P<0.01), NF-κB p65(P<0.01) changed significantly. CONCLUSIONS: The alteration of colonic permeability and increased expression of TNF-α, NF-κB p65 may play important roles in the occurrence and development of UC.