| 引用本文: | 叶晓莉,王丛瑶,刘汀,熊雪丰,吴梅君,王彬辉,李晴宇.冰片修饰的姜黄素阳离子脂质体的制备及其脑靶向作用研究[J].中国现代应用药学,2021,38(12):1469-1473. |
| YE Xiaoli,WANG Congyao,LIU Ting,XIONG Xuefeng,WU Meijun,WANG Binhui,LI Qingyu.Preparation of Curcumin-loaded Modifying Borneol Cationic Liposomes and Study on Its Brain Targeting Effect[J].Chin J Mod Appl Pharm(中国现代应用药学),2021,38(12):1469-1473. |
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| 冰片修饰的姜黄素阳离子脂质体的制备及其脑靶向作用研究 |
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叶晓莉1, 王丛瑶2, 刘汀1, 熊雪丰3, 吴梅君1, 王彬辉4, 李晴宇1
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1.浙江大学医学院附属杭州市第一人民医院临床药学科, 浙江省临床肿瘤药理与毒理学研究重点实验室, 杭州 310006;2.杭州市萧山区第一人民医院药学部, 杭州 311200;3.浙江医院药剂科, 杭州 310030;4.台州学院医学院附属市立医院药剂科, 浙江 台州 318000
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| 摘要: |
| 目的 制备冰片修饰的姜黄素阳离子脂质体（curcumin-loaded modifying borneol cationic liposomes，Cur-BCLPs），鼻腔给药后考察其在大鼠体内的药动学行为并对其脑组织分布进行研究。方法 采用乙醇注入法制备Cur-BCLPs；透射电镜观察阳离子脂质体的形态；激光粒度仪考察粒径；超速离心法测定其包封率及载药量；以姜黄素混悬液（curcumin suspension，Cur-Sol）和冰片-姜黄素混悬液（borneol curcumin suspension，BO-Cur-Sol）为对照组，考察大鼠鼻腔给药Cur-BCLPs的体内药动学过程，并测定其在大鼠脑组织的浓度，运用DAS 2.0软件拟合药动学参数。结果 阳离子脂质体外观呈圆形或类圆形，平均粒径为（105.99±2.40）nm，包封率和载药量分别为（81.95±1.03）%和（4.28±0.46）%；体内药动学结果显示，Cur-Sol、BO-Cur-Sol和Cur-BCLPs的半衰期（T1/2）分别为（4.27±1.53）h，（3.98±0.24）h和（6.01±0.63）h，AUC0→t分别为（224.38±21.95）μg·h·L-1，（243.40±12.26）μg·h·L-1和（562.28±24.30）μg·h·L-1，清除率分别为（1.82±0.36）L·h-1·kg-1，（1.72±0.11）L·h-1·kg-1和（0.78±0.03）L·h-1·kg-1，滞留时间分别为（4.28±0.23）h，（4.41±0.15）h和（8.09±0.17）h。脑组织分布结果显示，Cur-Sol、BO-Cur-Sol和Cur-BCLPs的AUC0→t分别为（29.82±1.10）μg·h·g-1，（35.47±1.75）μg·h·g-1和（54.06±3.90）μg·h·g-1，清除率分别为（15.73±0.84）L·h-1·kg-1，（13.23±0.52）L·h-1·kg-1和（8.52±0.92）L·h-1·kg-1。结论 Cur-BCLPs经鼻腔给药后显著提高姜黄素体内和脑组织蓄积量并且延缓消除。 |
| 关键词: 冰片|姜黄素|阳离子脂质体|药动学 |
| DOI：10.13748/j.cnki.issn1007-7693.2021.12.010 |
| 分类号:R969.1 |
| 基金项目:杭州市省市共建医学重点学科建设计划（浙卫办[2018]2号）；省级重点实验室资助项目（2020E10021）；杭州市医学重点学科资助项目（杭卫发[2021]21号）；浙江省中医药科技计划项目（2021ZA111）；浙江省卫生健康科技计划项目（2021KY865）；杭州市卫生科技计划项目（2018B013）；浙江省药学会医院药学专项科研基金项目（2020ZYY28，2012ZYY15） |
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| Preparation of Curcumin-loaded Modifying Borneol Cationic Liposomes and Study on Its Brain Targeting Effect |
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YE Xiaoli1, WANG Congyao2, LIU Ting1, XIONG Xuefeng3, WU Meijun1, WANG Binhui4, LI Qingyu1
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1.Department of Clinical Pharmacy, Key Laboratory of Clinical Cancer Pharmacology and Toxicology Research of Zhejiang Province, Affiliated Hangzhou First People's Hospital, Zhejiang University School of Medicine, Hangzhou 310006, China;2.Department of Pharmacy, The First People's Hospital of Xiaoshan District, Hangzhou 311200, China;3.Department of Pharmacy, Zhejiang Hospital, Hangzhou 310030, China;4.Department of Pharmacy, Medical College Affiliated Hospital of Taizhou University, Taizhou 318000, China
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| Abstract: |
| OBJECTIVE To prepare curcumin-loaded modifying borneol cationic liposomes(Cur-BCLPs), and to investigate their pharmacokinetics in vivo and the brain tissue distribution after intranasal administration. METHODS Cur-BCLPs were prepared with ethanol injection method; the morphology of cationic liposomes was observed by transmission electron microscope; mean particle size was estimated by laser particle size analyzer; entrapment efficiency and drug loading were investigated by ultracentrifugation; using curcumin suspension(Cur-Sol) and borneol curcumin suspension(BO-Cur-Sol) as control group, the pharmacokinetic behavior in vivo and the concentration in brain of Cur-BCLPs after intranasal administration in rats were studied. The pharmacokinetic parameters were calculated by DAS 2.0. RESULTS The shape of cationic liposomes was roundness. The mean particle size was (105.99±2.40)nm, entrapment efficiency was (81.95±1.03)%, drug loading was (4.28±0.46)%, respectively. Results of pharmacokinetic study in vivo showed that the T1/2 of Cur-Sol, BO-Cur-Sol and Cur-BCLPs were (4.27±1.53)h, (3.98±0.24)h and (6.01±0.63)h, AUC0→t were (224.38±21.95)μg·h·L-1, (243.40±12.26)μg·h·L-1 and (562.28±24.30)μg·h·L-1, clearance rate were (1.82±0.36)L·h-1·kg-1, (1.72±0.11)L·h-1·kg-1 and (0.78±0.03)L·h-1·kg-1,mean residence time were (4.28±0.23)h, (4.41±0.15)h and (8.09±0.17)h. Results of distribution in brain showed that AUC0→tof Cur-Sol, BO-Cur-Sol and Cur-BCLPs were (29.82±1.10)μg·h·g-1, (35.47±1.75)μg·h·g-1 and(54.06±3.90)μg·h·g-1, clearance rate were (15.73±0.84)L·h-1·kg-1, (13.23±0.52)L·h-1·kg-1and (8.52±0.92)L·h-1·kg-1. CONCLUSION Cur-BCLPs after intranasal administration may increase the concentration and slow their elimination in vivo and brain. |
| Key words: borneol|curcumin|cationic liposomes|pharmacokinetics |
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