神经毒素纳米粒的制备及在大鼠体内的组织分布  

Preparation of neurotoxin nanoparticles and tissue distribution in rats

作　　者：徐陆忠[1] 赵燕敏[1] 潘越芳[1] 魏颖慧[1] 李范珠[1] 

机构地区：[1]浙江中医药大学药学院,浙江杭州310053

出　　处：《中国医院药学杂志》2010年第17期1425-1428,共4页Chinese Journal of Hospital Pharmacy

基　　金：国家自然科学基金资助项目(编号:30772793)

摘　　要：目的:制备含冰片/薄荷脑低共熔物(BMEM)的神经毒素纳米粒(NT-NPs),并考察其体外性质和组织分布。方法:采用复乳-溶剂挥发法制备NT-NPs,通过光子相关光谱法和透析袋法分别考察其理化性质和体外释药特性;采用125I放射性同位素示踪法测定经大鼠鼻腔给药后在脑、心、肝、脾、肺及肾组织的放射性计数,并以每毫克组织的放射性计数表示组织分布情况。结果:纳米粒外观圆整,平均粒径为(76.1±30.8)nm,Zeta电位为(-29.2±3.1)mV,包封率为(70.6±4.3)%;体外释药呈现缓释和突释双相。与不含任何吸收促进剂组相比,BMEM组脑中的药量显著提高,增加了约19.11倍;其他各组织(除肺外)的药量亦有显著提高(P<0.01)。与冰片(BO)组相比,BMEM组脑和脾中的药量显著提高(P<0.05)。结论:含BMEM的NT-NPs包封率高,理化性质稳定,体外释药具有缓释特征。BMEM可有效增加NT-NPs经鼻腔吸收入脑及其他各组织的药量,是一种优良的新型吸收促进剂,具有良好的开发应用前景。OBJECTIVE To prepare NTNPs with BMEM and evaluate the characteristics in vitro and tissue dislribution in rats. METHODS The NTNPs were prepared by a modified double emulsion solvent evaporation method. The transmission e lectron microscope（TEM） and Zeta sizer instrument were utilized to investigam the physicochemical properties. The in vitro drug release behavior was studied by dialysis. The radioactive counts of 125 I-NT in brain, heart, liver, spleen, lung and kidney were determined by the method of radioisotope tracers. RESULTS The morphology of NTNPs with BMEM was spherical. The mean particle size,Zeta potential and entrapment efficiency of them were （76. 1 ±30. 8） nm, （ - 29.2 ± 3. 1 ）mV and （70. 6±4. 3）%, respectively. The in vitro release showed a significant sustained release after a brust release. The NT content in brain and other tissue（except lung） were significantly higher than that of NT-NPs without any absorption enhancers（P〈0.01 ）. And the group of NT-NPs with BMEM was higher than that of NTNPs with BO in brain and spleen（P〈0. 05）. CONCLUSION The NT-NPs with BMEM had high entrapment efficiency and good stability. The behavior of in witro release showed significant sustained release characteristics. BMEM can effectively increase the content of NT in brain and other tissues after i. n. administration and is a potential absorption enhancer.

关 键 词：神经毒素纳米粒 冰片/薄荷脑低共熔物 鼻腔给药 组织分布 大鼠 

分 类 号：R943[医药卫生—药剂学]