In recent years, organic-inorganic hybrid nanocarriers are explored for effective drug delivery and preferable disease treatments. In this study, using 5-fluorouracil(5-FU)as electronegative model drug, a new type of ...In recent years, organic-inorganic hybrid nanocarriers are explored for effective drug delivery and preferable disease treatments. In this study, using 5-fluorouracil(5-FU)as electronegative model drug, a new type of organic-inorganic hybrid drug delivery system(LDH/HA-PEG/5-FU)was conceived and manufactured by the adsorption of PEGylated hyaluronic acid(HA-PEG)on the surface of layered double hydroxide(LDH, prepared via hydrothermal method)and the intercalation of 5-FU in the interlamination of LDH via ion exchange strategy. The drug loading amount of LDH/HA-PEG/5-FU achieved as high as 34.2%. LDH, LDH/5-FU and LDH/HA-PEG/5-FU were characterized by FT-IR, XRD, TGA, laser particle size analyzer and SEM. With the benefit of p Hdegradable feature of LDH and enzyme-degradable feature of HA, LDH/HA-PEG/5-FU showed p H-degradable and enzyme-degradable capacity in in vitro drug release. Moreover, the drug carrier LDH/HA-PEG contained biocompatible PEG and tumor-targeted HA, resulting in lower cytotoxicity and better endocytosis compared with LDH in vitro. It was suggested that the organic-inorganic hybrid drug delivery system, which was endowed with the properties of controlled release, low toxicity and tumor-targeting delivery for ameliorative cancer therapy, was advisable and might be applied further to fulfill other treatments.展开更多
将含Arg-Gly-Asp(RGD)肽对多孔的PLGA-[ASP-PEG]表面进行改性,然后置于仿体液中两周,探讨肽改性的PLGA-(PEG-ASP)在仿体液中的矿化情况。通过交联剂Sulfo-LC-SPDP把肽接枝到PLGA-[ASP-PEG],X射线光电子能谱仪(X-ray photoelectron spect...将含Arg-Gly-Asp(RGD)肽对多孔的PLGA-[ASP-PEG]表面进行改性,然后置于仿体液中两周,探讨肽改性的PLGA-(PEG-ASP)在仿体液中的矿化情况。通过交联剂Sulfo-LC-SPDP把肽接枝到PLGA-[ASP-PEG],X射线光电子能谱仪(X-ray photoelectron spectroscopy,XPS)鉴定;肽改性PLGA-[ASP-PEG]为实验组(Experiment group,EG),PLGA-[ASP-PEG]为对照组(Control group,CG),均置于仿体液中两周,扫描电子显微镜(Scanning electron microscope,SEM)、X射线能谱仪(Energy dispersive analysis system of X-ray,EDS)及X射线衍射仪(X-ray diffractometry,XRD)对矿化情况进行分析。XPS检测肽改性PLGA-[ASP-PEG]表面硫元素结合能为164eV,碳、硫元素的含量比值(C/S)为99.746∶0.1014;SEM示在EG表面及内部呈现连续的较为致密的矿化层,CG仅见分散稀疏的矿化层;EDS及XRD结果表明矿化物主要成分为羟基磷灰石,EG矿化物中钙/磷比值为1.60,CG矿化物中钙/磷比值为1.52。含RGD肽为矿化提供了丰富的功能基团,PLGA-(PEG-ASP)经肽修饰矿化后,获得了与天然骨基质相似的微观结构。展开更多
基金Supported by the National Natural Science Foundation of China(No.81371667,No.31271073)
文摘In recent years, organic-inorganic hybrid nanocarriers are explored for effective drug delivery and preferable disease treatments. In this study, using 5-fluorouracil(5-FU)as electronegative model drug, a new type of organic-inorganic hybrid drug delivery system(LDH/HA-PEG/5-FU)was conceived and manufactured by the adsorption of PEGylated hyaluronic acid(HA-PEG)on the surface of layered double hydroxide(LDH, prepared via hydrothermal method)and the intercalation of 5-FU in the interlamination of LDH via ion exchange strategy. The drug loading amount of LDH/HA-PEG/5-FU achieved as high as 34.2%. LDH, LDH/5-FU and LDH/HA-PEG/5-FU were characterized by FT-IR, XRD, TGA, laser particle size analyzer and SEM. With the benefit of p Hdegradable feature of LDH and enzyme-degradable feature of HA, LDH/HA-PEG/5-FU showed p H-degradable and enzyme-degradable capacity in in vitro drug release. Moreover, the drug carrier LDH/HA-PEG contained biocompatible PEG and tumor-targeted HA, resulting in lower cytotoxicity and better endocytosis compared with LDH in vitro. It was suggested that the organic-inorganic hybrid drug delivery system, which was endowed with the properties of controlled release, low toxicity and tumor-targeting delivery for ameliorative cancer therapy, was advisable and might be applied further to fulfill other treatments.
文摘将含Arg-Gly-Asp(RGD)肽对多孔的PLGA-[ASP-PEG]表面进行改性,然后置于仿体液中两周,探讨肽改性的PLGA-(PEG-ASP)在仿体液中的矿化情况。通过交联剂Sulfo-LC-SPDP把肽接枝到PLGA-[ASP-PEG],X射线光电子能谱仪(X-ray photoelectron spectroscopy,XPS)鉴定;肽改性PLGA-[ASP-PEG]为实验组(Experiment group,EG),PLGA-[ASP-PEG]为对照组(Control group,CG),均置于仿体液中两周,扫描电子显微镜(Scanning electron microscope,SEM)、X射线能谱仪(Energy dispersive analysis system of X-ray,EDS)及X射线衍射仪(X-ray diffractometry,XRD)对矿化情况进行分析。XPS检测肽改性PLGA-[ASP-PEG]表面硫元素结合能为164eV,碳、硫元素的含量比值(C/S)为99.746∶0.1014;SEM示在EG表面及内部呈现连续的较为致密的矿化层,CG仅见分散稀疏的矿化层;EDS及XRD结果表明矿化物主要成分为羟基磷灰石,EG矿化物中钙/磷比值为1.60,CG矿化物中钙/磷比值为1.52。含RGD肽为矿化提供了丰富的功能基团,PLGA-(PEG-ASP)经肽修饰矿化后,获得了与天然骨基质相似的微观结构。
