目的 制备Angiopep-2(ANG)修饰的载神经毒素(neurotoxin, NT)介孔二氧化硅脂质囊纳米粒(mesoporous silica nanoparticles, MSN)(ANG-LP-MSN-NT),并进行体内外评价.方法 利用改进的Stober法制备介孔二氧化硅纳米粒,然后运用薄膜水化法制备ANG-LP-MSN-NT.考察其形态、粒径、Zeta电位、载药量和包封率;通过小角粉末衍射、氮气吸-脱附法等技术对其进行表征;透析袋法考察其体外释药特性;热板法和醋酸扭体法考察其镇痛效果.结果 制备的 MSN比表面积为557 m·g-1,孔径和孔容积(Vp)分别为2.94 nm和0.58 cm3·g-1.ANG-LP-MSN-NT分布均一,无团聚现象,粒径为(123.37士3.76) nm (PDI 0.20±0.02), Zeta 电位为(-16.57±1.59)mV,载药量与包封率分别为(10.75±0.54)％与 (91,82±3.12)％.ANG-LP-MSN-NT较MSN-NT体外突释降低,缓释特性明显;药效学实验结果表明ANG-LP-MSN-NT起效快、最大镇痛效应优于其他组别.结论 ANG-LP-MSN-NT解决了二氧化硅易团聚、易突释的问题,且更有利于NT在脑部富集,发挥更好的镇痛效果,该纳米递药系统作为神经毒素载体在镇痛方面具有较好的应用前景.“,”OBJECTIVE To prepare and evaluate Angiopep-2 (ANG) modifying neurotoxin (NT) loaded phospholipid-functionalized mesoporous silica nanoparticles (MSN) (ANG-LP-MSN-NT). METHODS MSN was synthesized by modified-Stober method. MSN-NT was developed by impregnation adsorption method. ANG-LP-MSN-NT was prepared by film hydration method. Laser particle size analyzer and transmission electron microscope were used to determine the particle size, Zeta potential and morphology. Small angle X-ray diffraction was used to determine the mesoporous structure; nitrogen adsorption method was used to calculate the surface area, pore diameter and pore volume. The drug release behavior of ANG-LP-MSN-NT was studied by dialysis method. Pharmacodynamics of ANG-LP-MSN-NT was studied by the hot-plate test and the acetic acid-writhing test. RESULTS The specific surface area, pore diameter and pore volume (Vp) of MSN were 557 m2·g-1, 2.94 nm and 0.58 cm3·g_1,respectively. The mean particle size and Zeta potential of ANG-LP-MSN-NT were (123.37±3.76)nm with PDI 0.20±0.02 and (-16.57±1.59)mV. The drug loading and entrapment efficiency of ANG-LP-MSN-NT were (10.75±0.54)％ and (91.82±3.12)％. In vitro release, compared with MSN-NT, burst release of ANG-LP-MSN-NT was smaller and sustained release was more obvious. The results of pharmacodynamics experiment showed that the onset time and the maximum effect of ANG-LP-MSN-NT were better than other groups. CONCLUSION The successful preparation of ANG-LP-MSN-NT solves the problem of aggregation and burst release of MSN and low drug loading and easy leakage of liposomes. ANG-LP-MSN-NT has profit for NT enrichment in brain and a better analgesic effect. ANG-LP-MSN is a prospective drug delivery system for neurotoxin.