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.

R283.6

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）