中国药理学通报
中國藥理學通報
중국약이학통보
CHINESE PHARMACOLOGICAL BULLETIN
2015年
8期
1136-1141
,共6页
项松涛%赵明%史现勋%付爱玲
項鬆濤%趙明%史現勛%付愛玲
항송도%조명%사현훈%부애령
姜黄素%RDP%脂质体%体内分布%细胞穿膜肽%脑靶向
薑黃素%RDP%脂質體%體內分佈%細胞穿膜肽%腦靶嚮
강황소%RDP%지질체%체내분포%세포천막태%뇌파향
curcumin%RDP%liposomes%biodistribu-tion%cell-penetrating peptides%brain targeting
目的以源于狂犬病毒糖蛋白的新型衍生肽( RVG-derived peptide, RDP)为靶向载体,研究其修饰的姜黄素隐形纳米脂质体的特征和脑靶向作用。方法薄膜分散法制备出脂质体。体外释放实验考察释药情况。小鼠经尾静脉注射姜黄素混悬液(CUR)、姜黄素脂质体(CUR-L)、RDP修饰的姜黄素隐形脂质体(RDP-CUR-L),分别在不同时间点取小鼠组织器官,HPLC法检测姜黄素在各组织的分布。结果制备的隐形纳米脂质体粒径在100 nm左右,分散性良好,包封率大于85%,制备重现性较好。小鼠经尾静脉分别注射CUR、CUR-L和 RDP-CUR-L后, CUR组并未在脑中检测到姜黄素, CUR-L 组仅在脑中检测到少量姜黄素,而RDP-CUR-L组小鼠脑内检测到了较高浓度的姜黄素。结论<br> RDP能够引导脂质体入脑,这将为治疗脑部疾病提供新的方法。
目的以源于狂犬病毒糖蛋白的新型衍生肽( RVG-derived peptide, RDP)為靶嚮載體,研究其脩飾的薑黃素隱形納米脂質體的特徵和腦靶嚮作用。方法薄膜分散法製備齣脂質體。體外釋放實驗攷察釋藥情況。小鼠經尾靜脈註射薑黃素混懸液(CUR)、薑黃素脂質體(CUR-L)、RDP脩飾的薑黃素隱形脂質體(RDP-CUR-L),分彆在不同時間點取小鼠組織器官,HPLC法檢測薑黃素在各組織的分佈。結果製備的隱形納米脂質體粒徑在100 nm左右,分散性良好,包封率大于85%,製備重現性較好。小鼠經尾靜脈分彆註射CUR、CUR-L和 RDP-CUR-L後, CUR組併未在腦中檢測到薑黃素, CUR-L 組僅在腦中檢測到少量薑黃素,而RDP-CUR-L組小鼠腦內檢測到瞭較高濃度的薑黃素。結論<br> RDP能夠引導脂質體入腦,這將為治療腦部疾病提供新的方法。
목적이원우광견병독당단백적신형연생태( RVG-derived peptide, RDP)위파향재체,연구기수식적강황소은형납미지질체적특정화뇌파향작용。방법박막분산법제비출지질체。체외석방실험고찰석약정황。소서경미정맥주사강황소혼현액(CUR)、강황소지질체(CUR-L)、RDP수식적강황소은형지질체(RDP-CUR-L),분별재불동시간점취소서조직기관,HPLC법검측강황소재각조직적분포。결과제비적은형납미지질체립경재100 nm좌우,분산성량호,포봉솔대우85%,제비중현성교호。소서경미정맥분별주사CUR、CUR-L화 RDP-CUR-L후, CUR조병미재뇌중검측도강황소, CUR-L 조부재뇌중검측도소량강황소,이RDP-CUR-L조소서뇌내검측도료교고농도적강황소。결론<br> RDP능구인도지질체입뇌,저장위치료뇌부질병제공신적방법。
Aim Targeted drug delivery in the brain is the necessary way for the treatment of brain diseases. In our study, a new peptide derived from the rabies vi-rus glycoprotein ( RVG-derived peptide, RDP ) was used as a targeted carrier to modify the curcumin stealth liposomes, and their characteristics and brain targeting effect were studied. Methods The curcumin liposomes were prepared by thin film dispersion. The release test in vitro was conducted to investigate their drug release. Curcumin distribution in several organs of mice was investigated by caudal vein injection of curcumin suspension liquid ( CUR ) , curcumin lipo-somes ( CUR-L) , RDP modified curcumin stealth lipo-somes ( RDP-CUR-L) via HPLC assay at different time points. Results The prepared stealth nano liposomes had a size of around 100 nm, and also had a good dis-persion and reproducibility. The entrapment efficiency was larger than 85%. After caudal vein injection of CUR, CUR-L and RDP-CUR-L in mice respectively, no curcumin was detected in brain of CUR group, and only a little was detected in CUR-L group. Neverthe-less, high concentration of curcumin was detected in RDP-CUR-L group. Conclusion RDP can deliver li-posome into the brain, which may provide a new meth-od for the treatment of brain diseases.
