Objective: This study was mainly focused on developing a dual-ligand liposomal delivery system to enhance both targeting specificity and cellular ***: The specific ligand transferrin (TF) and the cationic cell-penetra...
详细信息
Objective: This study was mainly focused on developing a dual-ligand liposomal delivery system to enhance both targeting specificity and cellular ***: The specific ligand transferrin (TF) and the cationic cell-penetrating peptide TAT were connected with cholesterol via a polyethylene glycol (PEG) spacer to prepare the dual-ligand liposomes (TAT/TF-PEG-LP).Then the in vitro cellular uptake by three kinds of cells that possessed different expressing levels of transferrin receptor (TFR) was *** Ex vivo fluorescence imaging of tumors,the qualitative observation of tumor frozen section and the quantitative determination of cellular uptake in tumor tissues were used to evaluate the in vivo delivery efficiency of TAT/***: The result of in vitro cellular uptake showed that TAT/TF-PEG-LP exhibited the enhanced cellular uptake and selectivity via the synergistic effect of both ligands in vitro compared to the single-ligand TAT or TF modified liposomes (TAT-PEG-LP or TF-PEG-LP),The ex vivo fluorescence imaging of tumors,the qualitative and quantitative evaluations of cellular uptake in tumor tissues altogether showed the in vivo delivery efficiency of TAT/TF-PEG-LP was higher than that of other ***: the dual-ligand liposomes co-modified with TF and TAT possessed a strong capability for synergistic targeted delivery of payload into tumor cells both in vitro and in vivo.
Breast cancer stem cells (BCSCs),which can fully recapitulate the tumor origin and are often resistant to chemotherapy and radiotherapy,are currently considered as a major obstacle for breast cancer *** achieve the go...
Breast cancer stem cells (BCSCs),which can fully recapitulate the tumor origin and are often resistant to chemotherapy and radiotherapy,are currently considered as a major obstacle for breast cancer *** achieve the goal of both targeting BCSCs and bulk breast cancer cells,we developed 8-hydroxyquinoline-loaded hyaluronan modified mesoporous silica nanoparticles (MSN)-supported lipid bilayers (HA-MSS) and docetaxel- loaded *** results showed that the size of all the nanoparticles was smaller than 200 *** were enriched from MCF-7 cells by a sphere formation method and identified with the CD44+/CD24- *** and qualitative analysis demonstrated that HA promotes the uptake of HA-MSS in CD44- overexpressing MCF-7 mammospheres,revealing the mechanism of receptor-mediated *** or DTX-loaded MSS showed much enhanced cytotoxicity against MCF-7 cells compared with MCF-7 mammospheres,whereas 8-HQ or 8-HQ-loaded HA-MSS showed much enhanced cytotoxicity against MCF-7 mammospheres compared with MCF-7 *** the MCF-7 xenografts in mice,the combination therapy with DTX-loaded MSS plus 8-HQ- loaded HA-MSS produced the strongest antitumor efficacy,with little systemic toxicity (reflecting by loss of body weight) in ***,this combination therapy may provide a potential strategy to improve the therapy of breast cancer by eradication of breast cancer cells together with BCSCs.
Objective To prepare insulin loaded chitosan nanoparticles (Ins-Cs-NPs),small intestine and colon specific delivery Ins-Cs-NPs loaded pellets and evaluate its oral pharmacodynamics *** Ins-Cs-NPs were prepared by the ...
详细信息
Objective To prepare insulin loaded chitosan nanoparticles (Ins-Cs-NPs),small intestine and colon specific delivery Ins-Cs-NPs loaded pellets and evaluate its oral pharmacodynamics *** Ins-Cs-NPs were prepared by the polyelectrolyte complexation method,then Ins-Cs-NPs was sprayed onto blank pellets core using Polyvinyl Pyrrolidone k30 as coating material to form Ins-Cs-NPs loaded *** intestine specific delivery was achieved by coating these pellets with Eudragit L30D-55,colon specific delivery was achieved by double-layer coating of chitosan and Eudragit *** appearance,particle size,encapsulation efficiency of Ins-Cs-NPs was observed and determined by relative instruments,the coating weight gain (CWG) of different pellets were optimized by dissolution test,the pharmacodynamics effects of all the preparation were evaluated by determing the plasma glucose level after *** The particle size was increased from (163.2±57.4) nm to (210.4±87.4)nm after solidified into pellets,and encapsulation efficiency decreased from (46.6±5.2)% to (42.9±6.8)%.Ins-Cs-NPs could partial protect insulin from degradation by pepsin or pancreatin within 1 *** test showed that 30% CWG of Eudragit L30D-55 could achieve good small intestine specific dedivery,and 40% CWG of chitosan combine with 30% CWG of Eudragit L100 controlled insulin almost unreleased in enzyme free medium but released when incubated with contents of colon in *** the subcutaneous injected groups showed significant hypoglycemic effect,however,all the oral groups neither nanoparticle suspension nor site specific pellets had such *** The particle size,encapsulation efficiency and bioactivity of insulin can be maintained when processed liquid Ins-Cs-NPs suspension into solid pellets by fluid-bed ***,the inherent structural defect of Ins-Cs-NPs made it less effective after oral administration wherever the gastric intestinal position they were delivered.
暂无评论