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作 者:申玉坤[1,2] 申玉璞[1] 潘一峰[2] 石春花[1] SHEN Yu-kun;SHEN Yu-pu;PAN Yi-feng;SHI Chun-hua(Changzhi Medical College,Changzhi 046000,China;Key Laboratory of Nanobiological Technology,Ministry of Health,Xiangya Medical College,Central South University,Changsha 41000& China)
机构地区:[1]长治医学院,山西长治046000 [2]中南大学湘雅医学院卫生部纳米生物技术重点实验室,湖南长沙410008
出 处:《中草药》2019年第12期2830-2834,共5页Chinese Traditional and Herbal Drugs
基 金:国家自然科学基金资助项目(81302075);长治医学院科研启动基金项目(QDZ201629);长治医学院博士启动基金资助项目(BS15015)
摘 要:目的合成新型的功能性氧化石墨烯-β-环糊精/多烯紫杉醇包合物(GO-DEX-β-CD/DOC)和四氧化三铁/氧化石墨烯-萘磺酸钠/多烯紫杉醇包合物(Fe3O4/GO-Na/DOC),并研究其对多烯紫杉醇(docetaxel,DOC)的装载、释放和经皮给药的渗透性能。方法以HPLC法测定DOC含量,并对制剂的高效装载和缓释性能进行研究,以离心法测定GO-DEX-β-CD/DOC和Fe3O4/GO-Na/DOC的包封率及载药率。将含药载体应用于离体和在体雌鼠皮肤,研究GO-DEX-β-CD/DOC和Fe3O4/GO-Na/DOC经雌鼠皮肤给药的渗透性。结果 Fe3O4/GO-Na/DOC的包封率和载药率更高,其释放具有较好的缓释性,经皮给药的渗透性能更好。结果显示,应用Fe3O4/GO-Na/DOC后90 h累积渗透量是(22.512±0.715)μg,15 min时皮肤内DOC浓度达峰值。给药5 h后,雌鼠血液中检测出DOC质量浓度达到(76.886±1.232)μg/mL。结论 Fe3O4/GO-Na/DOC制备工艺可行,其缓释性及透皮效果更好,具有广阔应用前景。Objective To synthetize the new-type GO-DEX-β-CD/DOC and Fe3O4/GO-Na/DOC inclusion compound, and study its high-efficiency loading, sustained-release and permeability as transdermal delivery for docetaxel (DOC) composites. Methods The concentration of DOC was determined by high efficiency liquid chromatography. The high-efficiency loading, sustained-release and permeability as transdermal delivery of GO-DEX-β-CD/DOC and Fe3O4/GO-Na/DOC were studied, and the encapsulation efficiency and drug loading of them were determined by centrifugation. The GO-DEX-β-CD/DOC and Fe3O4/GO-Na/DOC were applied onto the female mice skin in vitro and in vivo to develop the permeability of them. Results The encapsulation efficiency and drug loading of Fe3O4/GO-Na/DOC were higher than GO-DEX-β-CD/DOC, and its slow release property and permeability as transdermal delivery were better. The results showed that the accumulation permeation amount was (22.512 ±0.715)μg after Fe3O4/GO-Na/DOC being applied over 90 h, DOC concentration in skin reached a peak at 15 min by the application of Fe3O4/GO-Na/DOC. After 5 h of administration, DOC concentration in the blood of female mice reached (76.886 ±1.232)μg/mL. Conclusion The preparation techniques of Fe3O4/GO-Na/DOC was feasible with better sustained release and transdermal effect, which had a promising application prospect.
关 键 词:多烯紫杉醇 四氧化三铁/氧化石墨烯-萘磺酸钠/多烯紫杉醇包合物 功能性氧化石墨烯-β-环糊精/多烯紫杉醇包合物 经皮给药 缓释
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