咪喹莫特固体脂质纳米粒的制备及其性能研究  

Preparation and Characteristics of Imiquimod-Loaded Solid Lipid Nanoparticles

作　　者：周华锋[1] 马全红[1] 夏强[1] 陆杨燕[1] 缪旭[2] 顾宁[1] 骆丹[2] 

机构地区：[1]东南大学生物电子学国家重点实验室 [2]东南大学化学化工学院,南京210096

出　　处：《中国药学杂志》2006年第14期1084-1088,1120,共6页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(60171005;60371027);江苏省计划委员会资助项目(7607038009)

摘　　要：目的制备咪喹莫特固体脂质纳米粒,并考察其理化性质及其对透皮的影响。方法采用高压均质法制备咪喹莫特固体脂质纳米粒;采用透射电镜(TEM)观察纳米粒的形貌;光子相关光谱(PCS)测定其粒径大小和分布;紫外分光光度法测定载药纳米粒的包封率及载药量;MTT法进行细胞毒性试验,动态透析袋技术研究药物体外释放特性,采用Franz扩散法进行药物透皮试验。结果优化条件下制备的咪喹莫特固体脂质纳米粒平均粒径在(133±6)nm,多分散性指数(PI)值为0.348±0.05,平均包封率和载药量分别为(94.68±1.41)%和(4.73±0.07)%,体外释放呈现突释期和缓释释放期,对Hacat细胞无细胞毒性,增加了药物在皮肤层中的贮存量。结论咪喹莫特固体脂质纳米粒较优制备条件:癸酸与单硬脂酸甘油酯质量比为1∶3,S-40与Span-20质量比为1∶1;该咪喹莫特固体脂质纳米粒无皮肤刺激性,可望作为咪喹莫特经皮给药新制剂。OBJECTIVE To prepare imiquimod-loaded solid lipid nanoparticles and investigate their properties and transdermal permeation. METHODS IMQD-SLNs were prepared by high-pressure homogenization, single factor method was adopted to optimize the preparation parameters of IMQD-SLN. The morphology of IMQD-SLNs was observed by transmission electron microscope （TEM）. The mean diameter and size distribution were measured by photon correlation spectroscopy （PCS）. The entrapment capacity and drug loading were studied by UV spectro photometry. The cytotoxicity was researched by MTT method. RESULTS The mean diameter of optimized SLN was （ 133± 6） nm and polydispersity index （PI） was （0.348 ± 0.05） respectively. The entrapment capacity and content of drug loading were（94.68 ± 1.4） % and （4.73 ±0.07）%. No cytotoxicity was found in MTT experiment. A burst release was found in the initial 3 h followed by a continuous sustained release in vitro for IMQD-SLN. CONCLUSION The preparation of IMQD-SLN is optimized. The mass ratios of decanoic acid （DA）/ glycerol monostearate （GMS） and S-40/Span-20 are 1：3 and 1 ： 1, respectively. IMQD-SLNs might be a promiseful transdermal delivery system with no irritation to skin.

关 键 词：咪喹莫特 固体脂质纳米粒 毒性 体外释放 透皮 

分 类 号：R943.4[医药卫生—药剂学]